Cyclosporin A

别名: Cyclosporine A, Cyclosporine, Ciclosporin, CsA,NSC 290193 中文名称：环孢菌素A

目录号：S2286 Purity: 99.98%

Cyclosporin A, 一种非极性环寡肽，是一种免疫抑制剂，与亲环素结合，随后抑制calcineurin，无细胞试验中IC50为7 nM，广泛用于预防器官移植反应中的排斥反应,并已用于在灌注的3D近端小管模型上测试其毒性作用。Cyclosporin A (NSC 290193) 可用于诱导肝移植慢性排斥反应动物模型。

Cyclosporin A Chemical Structure

CAS: 59865-13-3

规格	价格	库存
10mM (1mL in DMSO)	1073.15	现货
50mg	786.07	现货
200mg	1957.41	现货
1g	5487.3	现货
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产品质控

批次：纯度： 99.98%

99.98

常与Cyclosporin A一起在实验中被使用的化合物

Diquafosol Tetrasodium

Cyclosporin A和Diquafosol Tetrasodium联合治疗可显着改善干眼症的客观体征和症状。

Eom Y, et al. J Ocul Pharmacol Ther. 2022 Dec;38(10):682-694.

Rapamycin

Cyclosporin A和Rapamycin对大鼠实验性自身免疫性葡萄膜视网膜炎(EAU)具有完全抑制作用。

Martin DF, et al. J Immunol. 1995 Jan 15;154(2):922-7.

Nifedipine

CyclosporinA和Nifedipine通过增加成纤维细胞和胶原密度引起大鼠牙龈过度生长。

Spoildorio LC, et al. J Periodontal Res. 2002 Jun;37(3):192-5.

Dexamethasone

Cyclosporin A和Dexamethasone可减少前列环素(PGI2)释放并增加纤溶酶原激活物抑制剂1(PAI-1)分泌。

Huang LQ, et al. Blood Coagul Fibrinolysis. 1995 Jul;6(5):438-45.

Selumetinib (AZD6244)

Cyclosporin A和Selumetinib组合在结直肠癌患者来源的肿瘤外植体(PDTX)模型中表现出肿瘤生长抑制和肿瘤消退。

Spreafico A, et al. Clin Cancer Res. 2013 Aug 1;19(15):4149-62.

Cyclosporin A相关产品

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相关化合物库	激酶抑制剂库 FDA药物库天然产物库已知活性药物库-I 高选择性抑制剂库	点击展开

细胞实验数据示例

细胞系	实验类型	给药浓度	孵育时间	活性描述	文献信息
human K562/R7 cells	Function assay	1 μM	72 h	Potentiation of doxorubicin-induced cytotoxicity against doxorubicin-resistant human K562/R7 cells assessed as doxorubicin IC50 at 1 uM after 72 hrs by MTT assay, IC50=0.7 μM	25634041
MDCK2	Function assay	10 uM	40 mins	Inhibition of human wild type Pgp expressed in MDCK2 cells assessed as calcein-AM accumulation at 10 uM after 40 mins.	17964170
C2C12	Function assay	0.1 ug/ml	3 days	Inhibition of hexose-6-phosphate dehydrogenase-induced cell differentiation in mouse C2C12 cells assessed as myosin heavy chain fluorescence at 0.1 ug/ml for 3 days.	20081855
HCT116	Function assay	10 uM	30 mins	Modulation of BCRP in human HCT116 cells assessed as intracellular accumulation of mitoxantrone at 10 uM after 30 mins by flow-cytometry.	21488686
2008	Function assay	10 uM	30 mins	Inhibition of human MRP1 expressed in 2008 cells at 10 uM preincubated for 30 mins prior to calcein AM addition measured every 60 secs up to 90 mins by calcein AM accumulation assay.	23017888
A2780adr	Function assay	10 uM	30 mins	Inhibition of human P-gp overexpressed in doxorubicin resistant A2780adr cells at 10 uM preincubated for 30 mins prior to calcein AM addition measured every 60 secs up to 90 mins by calcein AM accumulation assay.	23017888
HL60	Function assay	5 uM	40 mins	Inhibition of Ca2+-induced mitochondrial permeability transition in human HL60 cells at 5 uM after 40 mins relative to control.	23026083
Saos2	Function assay	5 uM	3 hrs	Inhibition of p-gp in doxorubicin-resistant human Saos2 cells assessed as increase in doxorubicin uptake at 5 uM after 3 hrs by flow cytometric analysis.	24720452
Saos2	Function assay	5 uM	2 hrs	Inhibition of p-gp in doxorubicin-resistant human Saos2 cells assessed as increase in intracellular doxorubicin retention at 5 uM after 2 hrs by flow cytometric analysis.	24720452
Saos2	Function assay	5 uM	2 to 3 hrs	Inhibition of p-gp in doxorubicin-resistant human Saos2 cells assessed as intracellular doxorubicin distribution in nuclei at 5 uM after 2 to 3 hrs by laser scanning confocal microscopic analysis.	24720452
A2780	Function assay	5 uM	40 mins	Inhibition of Pgp-mediated drug efflux in adriamycin-resistant human A2780 cells assessed as increase in intracellular adriamycin level at 5 uM after 40 mins by flow cytometry analysis.	24900323
A2780	Function assay	5 uM	1 hr	Inhibition of Pgp-mediated drug efflux in adriamycin-resistant human A2780 cells assessed as increase in adriamycin uptake at 5 uM after 1 hr by flow cytometry analysis.	24900323
A2780	Function assay	5 uM	8 hrs	Inhibition of Pgp-mediated drug efflux in adriamycin-resistant human A2780 cells assessed as increase in adriamycin uptake at 5 uM after 8 hrs by flow cytometry analysis.	24900323
T-cells	Antiinflammatory assay	0.01 to 100 nM	2 days	Antiinflammatory activity in LLO118 TCR transgenic mouse IL-2-competent CD4-positive T cells assessed as inhibition of LLO (190 to 205)-induced IL-2 production at 0.01 to 100 nM for 2 days by flow cytometric analysis.	24900866
Th17	Antiinflammatory assay	10 to 100 nM	2 days	Antiinflammatory activity in LLO118 TCR transgenic mouse Th17 cells assessed as inhibition of IL-17 production at 10 to 100 nM for 2 days by flow cytometric analysis.	24900866
Th1	Antiinflammatory assay	100 nM	2 days	Antiinflammatory activity in LLO118 TCR transgenic mouse Th1 cells assessed as inhibition of IFN-gamma production at 100 nM for 2 days by flow cytometric analysis.	24900866
CD1	Function assay	0.1 to 10 uM	30 mins	Inhibition of taurolithocholate acid 3-sulfate-induced necrosis in CD1 mouse pancreatic acinar cells at 0.1 to 10 uM after 30 mins by propidium iodide staining based confocal microscopic analysis.	26950392
Flp-InTM-293	Function assay	25 uM	30 mins	Inhibition of ABCC2 (unknown origin) expressed in human Flp-InTM-293 cells assessed as inhibition of calcein-AM efflux at 25 uM measured after 30 mins in presence of ABCB1 inhibitor GF120918 and ABCC1 inhibitor MK-571 by flow cytometry.	27393949
hamster BHK21	Function assay	25 uM	30 mins	Inhibition of human ABCC1 expressed in hamster BHK21 cells assessed as inhibition of calcein-AM efflux at 25 uM measured after 30 mins by flow cytometry.	27393949
MDCK2	Function assay	25 uM	30 mins	Inhibition of ABCC2 (unknown origin) expressed in MDCK2 cells assessed as inhibition of calcein-AM efflux at 25 uM measured after 30 mins in presence of ABCB1 inhibitor GF120918 and ABCC1 inhibitor MK-571 by flow cytometry.	27393949
NH3T3	Function assay	2.5 uM	30 mins	Inhibition of human ABCB1 expressed in mouse NH3T3 cells assessed as inhibition of calcein-AM efflux at 2.5 uM measured after 30 mins by flow cytometry.	27393949
MDA435/LCC6MDR	Function assay	1 uM	5 days	Inhibition of P-gp in human MDA435/LCC6MDR cells assessed as potentiation of paclitaxel-induced cytotoxicity by measuring paclitaxel IC50 at 1 uM measured after 5 days by Cell Titer 96 Aqueous assay (Rvb = 139.3 +/- 7.5 nM), IC50 = 0.0018 μM.	27750197
K562R	Function assay	5 uM	1 hr	Inhibition of P-gp in doxorubicin-resistant human K562R cells assessed as rhodamine efflux by measuring ratio of mean fluorescence intensity in presence and absence of compound at 5 uM incubated for 1 hr by flow cytometry.	27753480
HCT15	Function assay	0.4 to 6.3 ug/mL		Modulation of P-gp in human HCT15 cells assessed as increase in DINIB-induced cytotoxicity at 0.4 to 6.3 ug/mL.	11754602
UO31	Function assay	0.4 to 6.3 ug/mL		Modulation of P-gp in human UO31 cells assessed as increase in DINIB-induced cytotoxicity at 0.4 to 6.3 ug/mL.	11754602
CAKI1	Function assay	0.4 to 6.3 ug/mL		Modulation of P-gp in human CAKI1 cells assessed as increase in DINIB-induced cytotoxicity at 0.4 to 6.3 ug/mL.	11754602
HCT15	Function assay	10 uM		Inhibition of MDR1 in human HCT15 cells assessed as calcein-AM efflux at 10 uM by fluorescence assay.	21348461
mouse L5178 cells	Function assay		20 mins	Inhibition of human ABCB1-mediated rhodamine 123 efflux in mouse L5178 cells expressing human MDR1 after 20 mins by FACS analysis, IC50=0.65 μM	21341745
KB/MDR cell	Function assay		72 h	Inhibitory activity against KB/MDR cell line after 72 hr of drug exposure, IC50=1.5 μM	15481991
human MDA435/LCC6MDR cells	Cytotoxic assay		72h	Cytotoxicity against human MDA435/LCC6MDR cells expressing MDR after 72 hrs， IC50=2.8 μM	22320402
human Huh5-2 cells	Cytotoxic assay		3 days	Cytotoxicity against human Huh5-2 cells after 3 days by MTT assay , CC50=6 μM	18625766
human HuH6 cells	Cytotoxic assay		3 days	Cytotoxicity against human HuH6 cells after 3 days by MTT assay, CC50=7 μM	18625766
human Huh-9-13 cells	Cytotoxic assay		3 days	Cytotoxicity against human Huh-9-13 cells after 3 days by MTT assay， CC50=7 μM	18625766
african green monkey Vero cells	Function assay		24 h	Antiviral activity against West Nile virus infected in african green monkey Vero cells assessed as decrease in viral RNA synthesis after 24 hrs by luciferase reporter gene assay, IC50=8 μM	19451286
human LCC-6 cells	Cytotoxic assay		72 h	Cytotoxicity against human LCC-6 cells after 72 hrs, IC50=8.3 μM	22320402
human Huh-Mono cells	Cytotoxic assay		3 days	Cytotoxicity against human Huh-Mono cells after 3 days by MTT assay， CC50=24 μM	18625766
mouse L929 cells	Cytotoxic assay		3 days	Cytotoxicity against mouse L929 cells after 3 days by MTS assay, IC50=30 μM	25985195
human MDA435/LCC6MDR cells	Function assay		5 days	Modulation of P-gp (unknown origin) transfected in human MDA435/LCC6MDR cells assessed as reversing paclitaxel resistance measured as cell survival after 5 days by MTS assay, EC50=0.032 μM.	25985195
mouse T cells	Function assay		4 days	Immunosuppressive activity in mouse T cells assessed as inhibition of two way mixed lymphocyte reaction after 4 days by MTT assay, ic50=11 nM	22984987
human splenocytes	Function assay		4 days	Immunosuppressive activity in human splenocytes assessed as inhibition of [3H]thymidine incorporation after 4 days by allogenic mixed lymphocyte reaction assay, IC50=10 nM	19827831
human Jurkat cells	Function assay		1 h	Antiinflammatory activity in human Jurkat cells assessed as inhibition of anti-CD3/CD28 antibody-induced IL-2 production treated for 1 hr before anti-CD3/CD28 antibody challenge measured after 6 hrs by immunosuppression assay, EC50=5 nM	19933795
human PBMC	Function assay		1 h	Antiinflammatory activity in human PBMC assessed as inhibition of anti-CD3/CD28 antibody-induced IL-2 production treated for 1 hr before anti-CD3/CD28 antibody challenge measured after 6 hrs by immunosuppression assay, EC50=3.1 nM	19933795
PMBC	Function assay		72 hrs	Effect on proliferation of human peripheral blood mononuclear cells (PMBC) at 72 hr using MTT assay, IC50 = 8.97 μM.	15203163
A2780	Function assay		30 mins	Inhibition of human Pgp in A2780 cells after 30 mins by Hoechst 33342 assay, IC50 = 1.41254 μM.	18083034
A2780	Function assay		30 mins	Inhibition of human Pgp in A2780 cells after 30 mins by calcein AM assay, IC50 = 1.41254 μM.	18083034
Huh-9-13	Antiviral assay		3 days	Antiviral activity against BILN 2061-resistant HCV genotype 1b infected in human Huh-9-13 cells assessed as reduction in viral replication after 3 days by quantitative RT-PCR, EC50 = 0.004 μM.	19104013
Huh-9-13	Antiviral assay		3 days	Antiviral activity against compound-resistant HCV genotype 1b infected in human Huh-9-13 cells assessed as reduction in viral replication after 3 days by quantitative RT-PCR, EC50 = 0.35 μM.	19104013
Huh-9-13	Antiviral assay		3 days	Antiviral activity against 2'-C-methyl-2'-fluoro-cytidine-resistant HCV genotype 1b infected in human Huh-9-13 cells assessed as reduction in viral replication after 3 days by quantitative RT-PCR, EC50 = 0.4 μM.	19104013
Huh-9-13	Antiviral assay		3 days	Antiviral activity against VX 950-resistant HCV genotype 1b infected in human Huh-9-13 cells assessed as reduction in viral replication after 3 days by quantitative RT-PCR, EC50 = 0.49 μM.	19104013
Huh-9-13	Antiviral assay		3 days	Antiviral activity against R479-resistant HCV genotype 1b infected in human Huh-9-13 cells assessed as reduction in viral replication after 3 days by quantitative RT-PCR, EC50 = 1.98 μM.	19104013
Huh-9-13	Antiviral assay		3 days	Antiviral activity against cyclosporine-resistant HCV genotype 1b infected in human Huh-9-13 cells assessed as reduction in viral replication after 3 days by quantitative RT-PCR, EC50 = 3.85 μM.	19104013
HuH7	Antiviral assay		48 hrs	Antiviral activity against HCV subtype 1b Con1 infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by MTS assay, EC50 = 0.21 μM.	20176894
HuH7	Antiviral assay		48 hrs	Antiviral activity against cyclosporine A-resistant HCV subtype 1b Con1 infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by MTS assay, EC50 = 3.39 μM.	20176894
T-cells	Immunosuppressive assay		72 hrs	Immunosuppressive activity in BALB/c mouse T cells assessed as inhibition of anti-CD3/anti-CD28-stimulated cell proliferation after 72 hrs by MTT assay, IC50 = 0.06 μM.	21131104
T-cells	Cytotoxicity assay		48 hrs	Cytotoxicity against BALB/c mouse T cells after 48 hrs by MTT assay, CC50 = 15.82 μM.	21131104
T-cells	Immunosuppressive assay		96 hrs	Immunosuppressive activity in BALB/c/C57BL/6 mouse T cells assessed as inhibition of alloantigen-induced cell proliferation after 96 hrs by measuring [3H]thymidine uptake by mixed lymphocyte reaction assay, IC50 = 0.014 μM.	21456524
L929	Cytotoxicity assay		72 hrs	Cytotoxicity against mouse L929 cells after 72 hrs, IC50 = 33.9 μM.	22320402
CCRF-CEM/VCR1000	Function assay		240 secs	Inhibition of P-glycoprotein-mediated daunorubicin efflux from human CCRF-CEM/VCR1000 cells after 240 secs by FACS flow cytometric analysis, IC50 = 0.10233 μM.	22452412
mouse lymph node cells	Immunosuppressive assay		72 hrs	Immunosuppressive activity in anti-CD3/anti-CD8 co-stimulated Balb/c mouse lymph node cells assessed as inhibition of cell proliferation after 72 hrs by ELISA, IC50 = 0.07 μM.	22494616
mouse lymph node cells	Cytotoxicity assay		48 hrs	Cytotoxicity against Balb/c mouse lymph node cells after 48 hrs by MTT assay, CC50 = 10.1 μM.	22494616
HEK293	Function assay		5 mins	Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake incubated for 5 mins by scintillation counting, Ki = 1.2 μM.	22541068
HEK293	Function assay		5 mins	Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake incubated for 5 mins by scintillation counting, IC50 = 1.3 μM.	22541068
HEK293	Function assay		5 mins	Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake incubated for 5 mins by scintillation counting, Ki = 36 μM.	22541068
HEK293	Function assay		5 mins	Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake incubated for 5 mins by scintillation counting, IC50 = 37 μM.	22541068
T-cells	Immunosuppressive assay		24 hrs	Immunosuppressive activity in BALB/c mouse T cells assessed as inhibition of ConA-induced T cell proliferation incubated 24 hrs post ConA-induction for 72 hrs by MTT assay, IC50 = 2.12 μM.	22727369
RPMI1788	Immunosuppressive assay		6 days	Immunosuppressive activity in human RPMI1788 cells cocultured with human PBMC assessed as inhibition of [3H]thymidine incorporation incubated for 6 days prior to [3H]thymidine addition measured after 18 hrs by liquid scintillation counting, IC50 = 0.054 μM.	23347804
MT4	Antiviral assay		4 days	Antiviral activity against HIV1 3B infected in human MT4 cells coinfected with HTLV1 assessed as reduction in virus-induced cytopathogenicity after 4 days by MTT assay, EC50 = 0.45 μM.	23849880
A2780Adr	Function assay		30 mins	Inhibition of p-glycoprotein (unknown origin) expressed in human A2780Adr cells assessed as calcein-AM accumulation preincubated for 30 mins before calcein-AM addition measured up to 90 mins by fluorescence assay, IC50 = 0.99 μM.	23851114
2008	Function assay		30 mins	Inhibition of MRP1 (unknown origin) expressed in human 2008 cells assessed as calcein-AM accumulation preincubated for 30 mins before calcein-AM addition measured up to 90 mins by fluorescence assay, IC50 = 2.81 μM.	23851114
Jurkat T	Function assay		30 mins	Inhibition of NFAT activation in PMA/ionomycin-stimulated human Jurkat T cells incubated for 30 mins prior to PMA/ionomycin stimulation measured after 5 hrs by luciferase reporter gene assay, IC50 = 0.0014 μM.	23964991
MDA435/LCC6	Cytotoxicity assay		3 days	Cytotoxicity against human MDA435/LCC6 cells assessed as growth inhibition after 3 days by MTS assay, IC50 = 2.8 μM.	24171478
MDA435/LCC6MDR	Cytotoxicity assay		3 days	Cytotoxicity against human MDA435/LCC6MDR cells assessed as growth inhibition after 3 days by MTS assay, IC50 = 8.3 μM.	24171478
L929	Cytotoxicity assay		3 days	Cytotoxicity against mouse L929 cells assessed as growth inhibition after 3 days by MTS assay, IC50 = 33.9 μM.	24171478
A2780adr	Function assay		up to 90 mins	Inhibition of MDR1 in human doxorubicin-resistant A2780adr cells assessed as Calcein AM accumulation treated 30 mins before Calcein AM addition measured up to 90 mins by fluorescence assay, IC50 = 0.92 μM.	24184213
2008	Function assay		up to 90 mins	Inhibition of MRP1 in human 2008 cells assessed as Calcein AM accumulation treated 30 mins before Calcein AM addition measured up to 90 mins by fluorescence assay, IC50 = 2.7 μM.	24184213
NCI/ADR-RES	Function assay		20 mins	Inhibition of human P-glycoprotein expressed in NCI/ADR-RES cells assessed as reduction of calcein-AM transport after 20 mins by fluorescence assay.	24992153
A2780adr	Function assay		90 mins	Inhibition of ABCB1 in human A2780adr cells pre-incubated for 30 mins followed by calcein AM addition and further incubated for 60 mins by calcein AM assay, IC50 = 0.919 μM.	25855895
T spleen cells	Cytotoxicity assay		72 hrs	Cytotoxicity against ICR mouse T spleen cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, IC50 = 0.01 μM.	26564266
B spleen cells	Cytotoxicity assay		72 hrs	Cytotoxicity against ICR mouse B spleen cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, IC50 = 0.04 μM.	26564266
RD	Antiviral assay		24 hrs	Antiviral activity against EV71 infected in RD cells after 24 hrs by luciferase assay, EC50 = 3.66 μM.	26564266
A2780/ADR	Function assay		30 mins	Inhibition of ABCB1 in human A2780/ADR cells incubated for 30 mins measured up to 3600 secs with time intervals of 60 secs by calcein accumulation assay, IC50 = 1.41 μM.	27100033
A2780/ADR	Cytotoxicity assay		72 hrs	Cytotoxicity against human A2780/ADR cells overexpressing ABCB1 assessed as reduction in cell viability after 72 hrs by MTT assay, GI50 = 8.63 μM.	27100033
A2780	Cytotoxicity assay		72 hrs	Cytotoxicity against human A2780 cells assessed as reduction in cell viability after 72 hrs by MTT assay, GI50 = 8.94 μM.	27100033
Jurkat T	Immunosuppressive assay		13 hrs	Immunosuppressive activity in human PMA/ionomycin stimulated Jurkat T cells assessed as suppression of IL2 production pretreated with cells followed by PMA/ionomycin stimulation measured after 13 hrs by ELISA, IC50 = 0.011 μM.	27647370
A2780/ADR	Function assay		30 mins	Inhibition of ABCB1 in human A2780/ADR cells assessed as reduction in calcien-AM efflux preincubated for 30 mins followed by calcien-AM addition measured immediately at 60 sec time interval for 60 mins by fluorescence assay, IC50 = 1.21 μM.	27676469
HuH7	Antiviral assay		72 hrs	Antiviral activity against HCV genotype 1b Con1 infected in human HuH7 cells after 72 hrs by luciferase reporter gene assay, EC50 = 0.17 μM.	28075591
HepaRG	Antiviral assay		16 hrs	Antiviral activity against HBV infected in human HepaRG cells assessed as reduction in viral infection after 16 hrs, IC50 = 0.2 μM.	28383274
replicon 2A cells	Function assay		72 hrs	Inhibition of mTOR signaling pathway in (unknown origin) in sub-genomic replicon 2A cells assessed as reduction in phosphorylated rps6 protein levels up to 400 nM after 72 hrs by Western blot analysis.	28442256
A2780adr	Function assay		30 mins	Inhibition of ABCB1 in human A2780adr cells assessed as reduction in calcein AM levels preincubated for 30 mins followed by calcein AM addition measured immediately at 60 sec time interval for 60 mins by fluorescence assay, IC50 = 1.21 μM.	28471656
H69AR	Function assay		30 mins	Inhibition of ABCC1 in human H69AR cells assessed as reduction in calcein AM levels preincubated for 30 mins followed by calcein AM addition measured immediately at 60 sec time interval for 60 mins by fluorescence assay, IC50 = 2.97 μM.	28471656
A2780/ADR	Function assay		30 mins	Inhibition of ABCB1 in human A2780/ADR cells assessed as reduction in calcein-AM efflux preincubated for 30 mins followed by calcein-AM addition measured at 60 secs interval for 60 mins by fluorescence assay, IC50 = 1.21 μM.	28841513
H69AR	Function assay		30 mins	Inhibition of ABCC1 in human H69AR cells assessed as reduction in calcein-AM efflux preincubated for 30 mins followed by calcein-AM addition measured at 60 secs interval for 60 mins by fluorescence assay, IC50 = 3.53 μM.	28841513
C57BL/6 mouse lymph node cells	Immunosuppressive assay		24 hrs	Immunosuppressive activity in C57BL/6 mouse lymph node cells after 24 hrs by MTT assay, IC50 = 0.5 μM.	29871844
HuH7	Antiviral assay		3 days	Antiviral activity against HCV genotype 2a infected in human HuH7 cells after 3 days by dual-glo luciferase reporter gene assay, EC50 = 0.773 μM.	30074795
MT4	Cytotoxicity assay		4 to 5 days	Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 4 to 5 days by cell-titer glo assay, CC50 = 5.608 μM.	30074795
mouse mammary carcinoma cell line EMT6/AR 1.0	Function assay			Reversal effect on the accumulation of [3H]- daunorubicin in mouse mammary carcinoma cell line EMT6/AR 1.0, IC50=0.44 μM	10098671
KB cell	Function assay			Inhibitory activity against KB cell line after 72 h of drug exposure, IC50=0.6 μM	15481991
LLC-PK1 epithelial cells	Function assay			Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay， IC50=0.7 μM	12699389
A2780/ADR cells	Function assay			Inhibition of P-glycoprotein expressed in A2780/ADR cells by calcein AM assay， IC50=1.41254 μM	17890094
guinea pig ventricular myocytes	Function assay			Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes, IC50=2 μM	22761000
human Caco2 cells	Function assay			nhibition of P-gp in human Caco2 cells assessed as reduction in digoxin efflux, IC50=2.9 μM	23382458
leukemia CEM cells	Function assay			Inhibitory activity against Human MDR1 P-Glycoprotein ABC Transporter using leukemia CEM cells, IC50=3.4 μM	12361387
human HeLa cells	Function assay			Antiviral activity against HPV-18 infected in human HeLa cells assessed as inhibition of viral replication after 7 days， TC50=4.6 μM	18212100
human 2008 cells	Function assay			Inhibition of human MRP1 in human 2008 cells, IC50=4.78 μM	18707884
human HuH7 cells	Cytotoxic assay			Cytotoxicity against human HuH7 cells assessed as release of lactate dehydrogenase, IC50=5.81 μM	20943390
human HeLa cells	Cytotoxic assay			Cytotoxicity against human HeLa cells, TC50=8.3 μM	18212100
MDCK cells	Cytotoxic assay			Cytotoxicity against MDCK cells, TC50=9.9 μM	18212100
rat H42E cells	Cytotoxic assay			Cytotoxicity against rat H42E cells assessed as intracellular ATP level, TC50=42 μM	19502058
CK1 cells	Function assay			Antiviral activity against HPV-33 infected in CK1 cells assessed as inhibition of viral replication after 7 days, TC50=0.3 μM	18212100
HEK293 cells	Function assay			Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells assessed as protein-mediated pitavastatin uptake， Ki=0.2 μM	22587986
human PBMC	Proliferation assay			Antiproliferative activity against human PBMC, IC50=12 nM	15679309
human T-cell	Function assay			In vitro inhibitory activity against human T-cell production of lymphokine IL-2, IC50=8.1 nM	7537331
Jurkat cells	Function assay			Immunosuppressive activity was measured by inhibition of the IL-2 production in Jurkat cells, IC50=2 nM	14643337
HepG2 cells	Function assay			Inhibition of liver stage Plasmodium berghei infection in HepG2 cells, IC50=1.65 nM	22586124
Jurkat	Function assay			The compound was tested in vitro for inhibition of IL-2 release stimulated with PMA/ionomycin by Jurkat cells., IC50 = 0.012 μM.	7473543
mouse spleen cells	Function assay			The compound was tested in vitro for inhibition of proliferation in BDF1 mouse spleen cells stimulated with concanavalin A (ConA)., IC50 = 0.04 μM.	7473543
Sf9	Function assay			inhibition of Verapamil stimulated ATP hydrolysis in membranes from MDR1-expressing Sf9 cells, Ki = 0.02 μM.	7514263
LLC-PK1	Function assay			transepithelial transport (basal to apical) in MDR1-expressing LLC-PK1 cells, Km = 8.4 μM.	7681059
HeLa	Function assay			inhibition of LTC4 uptake in membrane vesicle from MRP1-expressing HeLa cells, Ki = 5 μM.	7961706
Caco-2	Function assay			transepithelial transport (basal to apical) in Caco-2 cells, Km = 3.8 μM.	8842452
spleen	Function assay			Effect of compound on IL-2 production from alloantigen-stimulated mouse spleen cells, IC50 = 0.01 μM.	8893839
COS	Function assay			inhibition of Taurocholate uptake in ASBT-expressing COS cells, Ki = 24 μM.	9458785
LLC-PK1	Function assay			inhibition of Doxorubicin transepithelial transport (basal to apical) (Digoxin: 0.8 uM) in MDR1-expressing LLC-PK1 cells, IC50 = 3.66 μM.	9914792
CEM/VLB100	Function assay			inhibition of Calcein-AM efflux in CEM/VLB100 cells, Ki = 1.8 μM.	10198227
HEK	Function assay			inhibition of BMG uptake in membrane vesicles from Mrp2-expressing HEK cells, Ki = 10 μM.	10421658
HEK	Function assay			inhibition of BMG uptake in membrane vesicles from MRP2-expressing HEK cells, Ki = 21 μM.	10421658
HeLa	Function assay			inhibition of Taurocholate uptake in NTCP-expressing HeLa cells, IC50 = 1 μM.	10565843
LLC-PK1	Function assay			inhibition of LTC4 uptake in membrane vesicles from MRP2-expressing LLC PK1 cells, Ki = 4.7 μM.	10570049
Sf9	Function assay			inhibition of Taurocholate uptake in membrane vesicles from Bsep-expressing Sf9 cells, Ki = 0.3 μM.	10648470
Caco-2	Function assay			inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 5 uM) in Caco-2 cells, IC50 = 1.3 μM.	10820137
CEM/VLB100	Function assay			inhibition of Calcein-AM efflux (Calcein-AM: 0.25 uM) in CEM/VLB100 cells, IC50 = 3.41 μM.	10891114
Sf9	Function assay			inhibition of ATPase in membrane vesicle from BCRP-expressing Sf9 cells, Ki = 0.5 μM.	11437380
NIH-3T3-G185	Function assay			inhibition of Daunorubicin efflux in NIH-3T3-G185 cells, IC50 = 1.4 μM.	11716514
NIH-3T3-G185	Function assay			inhibition of Calcein-AM efflux in NIH-3T3-G185 cells, IC50 = 1.7 μM.	11716514
NIH-3T3-G185	Function assay			inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells, IC50 = 1.7 μM.	11716514
NIH-3T3-G185	Function assay			inhibition of LDS-751 efflux in NIH-3T3-G185 cells, IC50 = 1.8 μM.	11716514
NIH-3T3-G185	Function assay			inhibition of Tetramethylrosamine efflux in NIH-3T3-G185 cells, IC50 = 2.1 μM.	11716514
NIH-3T3-G185	Function assay			inhibition of Fluo-3-AM efflux in NIH-3T3-G185 cells, IC50 = 2.4 μM.	11716514
NIH-3T3-G185	Function assay			inhibition of JC-1 efflux in NIH-3T3-G185 cells, IC50 = 4.3 μM.	11716514
MDA-435/LCC6 and MDA-435/LCC6-MDRI	Function assay			Concentration that reduces the difference in reversal of DOX accumulation between MDA-435/LCC6 and MDA-435/LCC6-MDRI cells by 50%., EC50 = 0.5 μM.	11784143
MDA-435/LCC6	Function assay			Effect on reversal of [3H]- VBL accumulation in MDA-435/LCC6 (Pgp-negative) cells., EC50 = 0.6 μM.	11784143
MDA-435/LCC6 and MDA-435/LCC6-MDRI	Function assay			Concentration that reduces difference in reversal of [3H]VBL accumulation between MDA-435/LCC6 and MDA-435/LCC6-MDRI cells by 50%, EC50 = 0.6 μM.	11784143
MDA435/LCC6 MDR1	Function assay			reversal of Vinblastine accumulation (Vinblastine: 0.005 uM) in MDA435/LCC6 MDR1 cells, EC50 = 0.6 μM.	11784143
MDA-435/LCC6 (Pgp-negative)	Function assay			Effect on reversal of DOX accumulation in MDA-435/LCC6 (Pgp-negative) cells., EC50 = 0.7 μM.	11784143
MDA-435/LCC6	Growth inhibitory assay			Growth inhibitory activity on MDA-435/LCC6 (Pgp-positive) human breast cancer cells., IC50 = 1 μM.	11784143
MDA-435/LCC6-MDRI	Growth inhibitory assay			Growth inhibitory activity on MDA-435/LCC6-MDRI (Pgp-negative) human breast cancer cells., IC50 = 1.1 μM.	11784143
BTI-TN5B1-4	Function assay			ATP hydrolysis in membrane fraction from High Five (BTI-TN5B1-4) cells, Km = 0.17 μM.	11785684
Jurkat	Function assay			Inhibition of production of IL-2 secretion in Jurkat cells, IC50 = 0.007 μM.	11881984
Jurkat	Function assay			Inhibition of production of beta-galactosidase IL-2 RGA in Jurkat cells, IC50 = 0.008 μM.	11881984
LLC-PK1	Function assay			increase in Vinblastine intracellular accumulation in MDR1-expressing LLC-PK1 cells, Ki = 1.3 μM.	11961113
LLC-PK1	Function assay			increase in Calcein-AM intracellular accumulation in MDR1-expressing LLC-PK1 cells, Ki = 4.66 μM.	11961113
MDCK	Function assay			inhibition of Digoxin transepithelial transport (basal to apical) in MDR1-expressing MDCK cells, Ki = 2.18 μM.	12134945
MDCK	Function assay			inhibition of Vinblastine transepithelial transport (basal to apical) in MRP2-expressing MDCK cells, Ki = 8.11 μM.	12134946
LLC-PK1	Function assay			increase in Calcein-AM intracellular accumulation in mdr1b-expressing LLC-PK1 cells, Ki = 3.5 μM.	12235267
LLC-PK1	Function assay			increase in Calcein-AM intracellular accumulation in mdr1a-expressing LLC-PK1 cells, Ki = 3.65 μM.	12235267
HL-60	Function assay			Inhibitory activity against Human formylpeptide receptor (FPR) of human leukemia HL-60 cells, IC20 = 3.6 μM.	12361388
High Five cells	Function assay			inhibition of Taurochenodeoxycholate uptake(CsA 30uM, 30 % of control) in membrane vesicles prepared from High Five cells infected with the ABCB11 baculovirus, Ki = 9.5 μM.	12404239
MDCKII	Function assay			inhibition of Cerivastatin uptake in OATP2-expressing MDCKII cells, Ki = 0.238 μM.	12538813
Caco-2	Function assay			transepithelial transport of digoxin (basal to apical) in Caco-2 cells, Ki = 0.35 μM.	12636153
SK-E2	Function assay			increase in bodipy intracellular accumulation (Bodipy: 0.2 uM) in SK-E2 cells (expressing BSEP), IC50 = 7.5 μM.	12739759
SK-E2	Function assay			increase in dihydrofluorescein intracellular accumulation (dihydrofluorescein: 1 uM) in SK-E2 cells (expressing BSEP), IC50 = 7.8 μM.	12739759
HEK293	Function assay			inhibition of Phalloidin uptake (Phalloidin: 1 uM) in OATP-C-expressing HEK293 cells, Ki = 0.2 μM.	14530907
T-cells	Function assay			Inhibition of allogenic cells-stimulated proliferation in mouse T cells by mixed lymphocyte reaction method, IC50 = 0.032 μM.	14593182
T-cells	Function assay			Inhibition of allogenic cells-stimulated proliferation in human T cells by mixed lymphocyte reaction method, IC50 = 0.074 μM.	14593182
mouse spleen cells	Cytotoxicity assay			Cytotoxicity against BALB/c mouse spleen cells, CC50 = 1.35 μM.	17081761
MDCK2	Function assay			Inhibition of human MDR1-dependent accumulation of calcein-AM expressed in MDCK2 cells, IC50 = 9.34 μM.	17664327
HEK293	Function assay			Inhibition of cross-linking of human Pgp TM1 L65R/TM6 L339C/TM7 F728 mutant expressed in HEK293 cells assessed as drug level causing 50% inhibition of cross linking by immunoblot, Activity = 0.5 μM.	17848563
HEK293	Function assay			Inhibition of cross-linking of human Pgp TM6 L339C/TM7 F728C mutant expressed in HEK293 cells assessed as drug level causing 50% inhibition of cross linking by immunoblot, Activity = 0.6 μM.	17848563
HEK293	Function assay			Inhibition of cross-linking of human Pgp TM3T199R/TM6 L339C/TM7 F728C mutant expressed in HEK293 cells assessed as drug level causing 50% inhibition of cross linking by immunoblot, Activity = 1.1 μM.	17848563
HEK293	Function assay			Inhibition of cross-linking of human Pgp TM6 F343R/TM6 L339C/TM7 F728C mutant expressed in HEK293 cells assessed as drug level causing 50% inhibition of cross linking by immunoblot, Activity = 11 μM.	17848563
HEK293	Function assay			Inhibition of cross-linking of human Pgp TM5 I306R/TM6 L339C/TM7 F728C mutant expressed in HEK293 cells assessed as drug level causing 50% inhibition of cross linking by immunoblot, Activity = 15 μM.	17848563
Caco-2	Function assay			Inhibition of P-glycoprotein-mediated [3H]vinblastine transport in human Caco-2 cells, EC50 = 45.5 μM.	18524592
A2780	Function assay			Inhibition of P-gp in human adriamycin-resistant A2780 cells by Hoechst 33342 assay, IC50 = 1.41254 μM.	18678495
A2780/ADR	Function assay			Inhibition of P-glycoprotein-mediated multidrug resistance in adriamycin-resistant human A2780/ADR cells by calcein AM assay, IC50 = 1.4 μM.	19250834
C2C12	Function assay			Inhibition of serum withdrawal-induced cell differentiation in mouse C2C12 cells assessed as myosin heavy chain expression.	20081855
mouse spleen cells	Function assay			Inhibition of serine palmitoyltransferase in mouse spleen cells.	21456524
Sf21	Function assay			Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake, IC50 = 0.5 μM.	21965623
Sf21	Function assay			Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake, IC50 = 0.6 μM.	21965623
T-cells	Function assay			Inhibition of CD4 expression in human CD4+ T cells, IC50 = 8.97 μM.	22101135
HEK293	Function assay			Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake by scintillation counting, Ki = 1.3 μM.	22541068
HEK293	Function assay			Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake by scintillation counting, IC50 = 1.4 μM.	22541068
MDA435/LCC6MDR	Function assay			Modulation of p-gp (unknown origin) transfected in human MDA435/LCC6MDR cells assessed as reversal of paclitaxel resistance, EC50 = 0.032 μM.	24171478
mouse	Function assay			Inhibition of human MDR1 expressed in mouse L5178 cells assessed as increase in intracellular accumulation of rhodamine 123 by FACSCalibur flow cytometry, IC50 = 0.67 μM.	24900226
mouse lymph node cells	Function assay			Inhibition of PI3K-gamma in mouse lymph node cells assessed as inhibition of ConA-stimulated T cell proliferation, IC50 = 0.57 μM.	26720154
MDCK2	Function assay			Inhibition of ABCC2 (unknown origin) expressed in MDCK2 cells assessed as inhibition of calcein-AM efflux measured after 30 mins in presence of ABCB1 inhibitor GF120918 and ABCC1 inhibitor MK-571 by flow cytometry, IC50 = 25.6 μM.	27393949
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells.	29435139
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells.	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells.	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells.	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells.	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells.	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells.	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells.	29435139
Rh30	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells.	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells.	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells.	29435139
Rh18	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells.	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells.	29435139
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells.	29435139
点击查看更多细胞系数据

生物活性

产品描述

靶点

calcineurin ^[1]
(Cell-free assay)

7 nM

体外研究(In Vitro)
体外研究活性	在T细胞中，Cyclosporin A与亲环蛋白(免疫亲和素)结合^[1]，形成亲环蛋白-Cyclosporin A复合体，其结合并抑制钙调磷酸酶。^[2]Cyclosporin A 抑制钙调磷酸酶，IC50 是7 nM^[3]，随后阻断NF-AT核转运。 ^[4]Cyclosporin A通过抑制MTP(线粒体通透性转换孔)的开放而影响线粒体，IC50 是39 nM。^[5]
激酶实验	磷酸酶试验
激酶实验	纯化的牛脑钙调磷酸酶和钙调蛋白是购买的。含纯化酶的反应混合物包含100 nM 钙调磷酸酶，100 nM 钙调蛋白，以及5 μM ³²P-标记磷酸化多肽，60 μl (总体积) 试验缓冲液包含20 mM Tris (pH 8)，100 mM NaCI，6 mM MgCl₂，0.5 mM 二硫苏糖醇，每毫升0.1毫克牛血清白蛋白，以及0.1 mM CaCl₂或5 mM EGTA。含细胞裂解物的反应混合物包含20 μl of未稀释裂解物， 5 μM ³²P-标记的磷酸肽，和40 μl 试验缓冲液。反应混合物包含50 μM 多肽412或413和/或 500 nM冈田酸，一种磷酸酶1和2A的特异性抑制剂; 500 nM 冈田酸足以抑制Ca²⁺-不依赖性磷酸酶，而更高浓度时也会部分抑制Ca²⁺-依赖性的活性。30°C下培育15分钟，加入0.5 ml包含5% 三氯乙酸的100 mM 磷酸钾缓冲液(pH 7.0)终止反应。Dowex阳离子交换色谱分离无机磷酸盐，用闪烁计数测定数量。
细胞实验	细胞系	Jurkat细胞(无性繁殖J77)
	浓度	~100 nM
	孵育时间	1小时
	方法	免疫抑制剂以细胞治疗浓度的1000倍溶于乙醇。细胞(10⁶)悬浮于微量离心管1ml完全培养基中；1 μl乙醇或者Cyclosporin A乙醇溶液加入反应液中，细胞在37°C下培育1小时。细胞在冰浴下用1ml PBS洗两次，在50μl低渗缓冲液中裂解，缓冲液每毫升包含50 mM Tris (pH 7.5); 0.1 mM EGTA; 1 mM EDTA; 0.5 mM二硫苏糖醇; 以及50 微克苯甲基磺酰氯，50 微克胰蛋白酶抑制剂，5微克亮抑酶肽，和5 微克抑肽酶。裂解液用液氮冷冻，再在30°C下融化，循环3次，随后在 4°C下以12,000×g离心10分钟。
实验图片	检测方法	检测指标	实验图片	PMID
	Western blot	Phospho-AKT1 / AKT1 / PTEN / Phospho-BAD / BAD / Procaspase-3 Cyp-D / AIF / β-actin IL-8 / MCP-1 Actin / Smac β-actin / FIPV-N		12644839
	Growth inhibition assay	NPC death		20181586
	IHC	Th22 / Th17 / Th1 / M1 / Th2 Tregs / Bregs / pDCs / M2 Ki 67 / Fas-FasL IFN-γ / TNF-α WT-PCLS / FXRKO-PCLS		30916387
	Immunofluorescence	Human gingival fibroblast cells Human gingival fibroblast cells Calcein Rhod-Dex / Calcein cadherin-9 / vimentin		27857765

体内研究(In Vivo)
体内研究活性	Cyclosporin A是一种免疫抑制剂，小鼠，大鼠，和荷兰猪经非肠道给药或者口服给药都有效^[6]，临床上用于器官移植中预防免疫排斥。^[7]
动物实验	Animal Models	大鼠
	Dosages	45毫克/千克
	Administration	口服

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
临床试验信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT06366685	Not yet recruiting	Esophageal Cancer\|Exercise Training\|Psychotherapy\|Rehabilitation	Mengmeng Yuan\|Anhui Medical University	May 1 2024	Not Applicable
NCT06320561	Not yet recruiting	Stroke	Vrije Universiteit Brussel\|University Ghent\|Research Foundation Flanders	May 2024	--
NCT05702931	Not yet recruiting	Hyperglycemia\|Renal Transplant Complication Primary Non-Function\|Diabetes	Rigshospitalet Denmark\|Aarhus University Hospital\|Odense University Hospital	April 1 2024	Phase 4
NCT06052761	Recruiting	Child in Hospital	Adiyaman University	February 10 2024	Not Applicable

参考文献
[1] Handschumacher RE, et al. Science, 1984, 226(4674), 544-547. [2] Liu J, et al. Cell, 1991, 66(4), 807-815. [3] Fruman DA, et al. PNAS, 1992, 89(9), 3686-3690. [4] Flanagan WM, et al. Nature, 1991, 352(6338), 803-807. [5] Nicolli A, et al. J Biol Chem, 1996, 271(4), 2185-2192. [6] Borel JF, et al. Immunology, 1977, 32(6), 1017-1025. [7] Williams, R, et al. Lancet, 1994, 344(8920), 423-428. [8] https://link.springer.com/chapter/10.1007/978-94-011-0679-5_12 [9] Homan KA, et al. Sci Rep. 2016 Oct 11;6:34845. + 展开

参考文献

+ 展开

化学信息&溶解度

分子量	1202.61	分子式	C₆₂H₁₁₁N₁₁O₁₂
CAS号	59865-13-3	SDF	Download Cyclosporin A SDF
Smiles	CCC1C(=O)N(CC(=O)N(C(C(=O)NC(C(=O)N(C(C(=O)NC(C(=O)NC(C(=O)N(C(C(=O)N(C(C(=O)N(C(C(=O)N(C(C(=O)N1)C(C(C)CC=CC)O)C)C(C)C)C)CC(C)C)C)CC(C)C)C)C)C)CC(C)C)C)C(C)C)CC(C)C)C)C
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

体外溶解度
批次：

DMSO : 100 mg/mL ( (83.15 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Ethanol : 100 mg/mL (83.15 mM)

Water : Insoluble

DMSO : 100 mg/mL ( (83.15 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Ethanol : 100 mg/mL (83.15 mM)

Water : Insoluble

DMSO : 100 mg/mL ( (83.15 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Ethanol : 100 mg/mL (83.15 mM)

Water : Insoluble

摩尔浓度计算器

体内溶解配方批次：现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂				动物体内配方计算器
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
澄清溶液	2%DMSO 1 40%PEG300 2 5%Tween80 3 53%ddH2O 该配方已经过Selleck实验室实测。如果上述溶解方案不能满足您的需求，可联系Selleck销售提供定制化测试。	2.500mg/ml (2.08mM)	以 1 mL 工作液为例，取20μL125mg/ml的澄清DMSO储备液加到400μL PEG300中，混合均匀使其澄清；向上述体系中加入50μLTween80，混合均匀使其澄清；然后继续加入530μL ddH2O定容至 1 mL。工作液请现配现用！
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
澄清溶液	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O 该配方已经过Selleck实验室实测。如果上述溶解方案不能满足您的需求，可联系Selleck销售提供定制化测试。	5.000mg/ml (4.16mM)	以 1 mL 工作液为例，取50μL100mg/ml的澄清DMSO储备液加到 400μL PEG300中，混合均匀使其澄清；向上述体系中加入50μLTween80，混合均匀使其澄清；然后继续加入500μL ddH2O定容至 1 mL。工作液请现配现用！
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。

实验计算

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

动物体内配方计算器（澄清溶液）

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

计算结果：

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH₂O，混匀澄清。

体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。

注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

技术支持

在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题，请给我们留言。

* 必填项

常见问题及建议解决方法

问题 1:
What is the difference between S2286 (cyclosporin A) and S1514 (cyclosporin)?

回答：
Cyclosporine is a mixture of Cyclosporine A, derivatives of Cyclosporine A, salts of Cyclosporine A. Cyclosporine A is an especially useful Cyclosporine component.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):