Tacrolimus (FK506)
别名: FR900506, Fujimycin 中文名称：他克莫司
Tacrolimus (FK506) 是一种23元大环内酯物，通过结合到抑免蛋白FKBP12 (FK506 结合蛋白)产生新的复合物，从而降低T细胞中肽酰脯氨酰异构酶活性。Tacrolimus 也可抑制calcineurin钙调磷酸酶的磷酸酶活性。Tacrolimus 可诱导血管内皮细胞的自噬。
Tacrolimus (FK506) Chemical Structure
CAS: 104987-11-3
产品质控
批次：
纯度：
99.97%
99.97
Tacrolimus (FK506)相关产品
| 相关靶点 | FKBP1 FKBP12 | 点击展开 |
|---|---|---|
| 相关产品 | Shield-1 AP20187 | 点击展开 |
| 相关化合物库 | 激酶抑制剂库 PI3K/Akt 抑制剂库 凋亡分子化合物库 细胞周期化合物库 NF-κB信号通路库 | 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 |
|---|---|---|---|---|---|
| rat RBL2H3 cells | Function assay | 15 mins | Antiinflammatory activity in rat RBL2H3 cells assessed as inhibition of DNP-BSA-induced TNF-alpha production preincubated for 15 mins prior DNP-BSA challenge measured after 30 mins by ELISA, IC50=0.25 nM | 22410084 | |
| rat RBL2H3 cells | Function assay | 16 h | Inhibition of TNF-alpha production in rat RBL2H3 cells after 16 hrs by ELISA, IC50=0.25 nM | 23791076 | |
| Jurkat T | Immunosuppressive assay | 15 to 30 mins | Immunosuppressive activity in PMA/ionomycin stimulated human Jurkat T cells assessed as suppression of IL2 production pretreated for 15 to 30 mins followed by PMA/ionomycin addition measured after 18 to 20 hrs by ELISA, IC50 = 0.36 μM. | 28412204 | |
| Jurkat T | Antiinflammatory assay | 20 mins | Anti-inflammatory activity in PMA/ionomycin stimulated human Jurkat T cells assessed as reduction in IL-2 secretion preincubated for 20 mins followed by PMA/ionomycin stimulation measured after 12 hrs by ELISA, IC50 = 5.8 μM. | 28509552 | |
| human T-cell | Proliferation assay | In vitro inhibitory activity against human T-cell proliferation, IC50=0.5 nM | 7537331 | ||
| human WiDr cells | Growth inhibition assay | Inhibition of SAP130 mediated cell growth in human WiDr cells, IC50=10.9 nM | 17643112 | ||
| human U251 cells | Function assay | Inhibition of SAP130 in VEGF-stimulated human U251 cells by PLAP reporter gene assay, IC50=13.8 nM | 17643112 | ||
| PBMCs | Function assay | Inhibitory activity against IFN-gamma production (Anti-CD3 monoclonal antibody stimulated and cultured CD4 positive cells purified from human peripheral blood mononuclear cell), IC50 = 0.00006 μM. | 15369399 | ||
| PBMCs | Function assay | Inhibitory activity against IL-5 production (Anti-CD3 monoclonal antibody stimulated and cultured CD4 positive cells purified from human peripheral blood mononuclear cell), IC50 = 0.00006 μM. | 15369399 | ||
| T-cells | Function assay | The compound was tested for its inhibitory activity against T-cell proliferation using murine splenic T-cells, IC50 = 0.0002 μM. | 10450987 | ||
| RBL-2H3 | Function assay | Inhibition of DNP7-BSA antigen-induced TNFalpha release in rat RBL-2H3 cells, IC50 = 0.00025 μM. | 16901696 | ||
| HEK293 | Function assay | TP_TRANSPORTER: inhibition of Phalloidin uptake (Phalloidin: 1 uM) in OATP-C-expressing HEK293 cells, IC50 = 3.7 μM. | 14530907 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Tacrolimus (FK506) 是一种23元大环内酯物，通过结合到抑免蛋白FKBP12 (FK506 结合蛋白)产生新的复合物，从而降低T细胞中肽酰脯氨酰异构酶活性。Tacrolimus 也可抑制calcineurin钙调磷酸酶的磷酸酶活性。Tacrolimus 可诱导血管内皮细胞的自噬。 | ||
|---|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | FK-506和环孢霉素A阻断细胞质成分的移位，而不影响T淋巴细胞中核亚基的合成。[1] FK-506通过抑制需要白细胞介素-2转录诱导的Ca(2+)-依赖过程，阻止T细胞增殖。[2] FK 506结合于不同的细胞内蛋白质(免疫亲和素)家族，学术上称为亲环素类和FK 506结合蛋白(FKBPs)。FK-506特异性抑制细胞内磷酸酶，在药物浓度下，抑制活化的T细胞中白介素2的产生。[3] FK-506和CsA通过抑制早期钙相关的涉及淋巴因子表达，凋亡，和脱粒作用，在细胞中几乎发挥相同的生物学作用。FK-506与细胞内受体家族结合，学术上称为FK-506结合蛋白(FKBPs)。[4] |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | GluA1 / pGluA1(S845) / GluA2 / GluA3 / Calcineurin p-JNK / JNK / p-ERK / ERK / Cytochrome c / cleaved caspase-3 p-S6K(S371) / S6K / p-Erα(S167) / Erα |
|
26455952 | |
| Immunofluorescence | FKBP52 / p23 / hsp90 FKBP51 Tom20 / JC-1 / ROS / NF-κB |
|
20796173 | |
| Growth inhibition assay | Cell viability |
|
23470533 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | 大鼠行为疼痛评估中，FK-506导致痛觉过敏和异常疼痛刺激下爪子和尾巴收缩的阈值增加。在大鼠体内，FK-506也会导致血清硝酸盐和硫代巴比妥酸活性产物(TBARS)水平降低，并伴随组织髓过氧化物酶(MPO)和总钙水平降低，然而，会升高组织中还原型谷胱甘肽的水平。在缺血再灌注损伤(I/R)的大鼠体内，FK-506可以改善加重的神经水肿和轴突变性。[5] |
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|---|---|---|
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| 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 |
| NCT06268769 | Recruiting | Immunosuppression |
Edward Geissler|Chiesi Pharmaceuticals GmbH|University of Regensburg |
March 9 2024 | Phase 4 |
| NCT06326775 | Active not recruiting | Heart Transplant Patients |
Nanjing First Hospital Nanjing Medical University|Wuhan Union Hospital China|Changhai Hospital|Shanghai Zhongshan Hospital |
March 12 2024 | -- |
| NCT06235892 | Not yet recruiting | Organ Grafts |
Nantes University Hospital |
February 10 2024 | Phase 3 |
化学信息&溶解度
| 分子量 | 804.02 | 分子式 | C44H69NO12 |
| CAS号 | 104987-11-3 | SDF | Download Tacrolimus (FK506) SDF |
| Smiles | CC1CC(C2C(CC(C(O2)(C(=O)C(=O)N3CCCCC3C(=O)OC(C(C(CC(=O)C(C=C(C1)C)CC=C)O)C)C(=CC4CCC(C(C4)OC)O)C)O)C)OC)OC | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 100 mg/mL ( (124.37 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 100 mg/mL (124.37 mM) Water : Insoluble |
摩尔浓度计算器 |
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体内溶解配方 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 | |||||
实验计算
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）
mg/kg
g
μL
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。
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常见问题及建议解决方法
问题 1:
we would like to inject it subcutaneously into rats, Can we mix the FK506 with 5% dextrose to a concentration of 5mg/ml to prepare the solution?
回答：
You can dissolve FK506 with DMSO to prepare the stock solution, and then dilute by 5% dextrose. However, we don't have the information about the solubility in this condiation. Or you can use the vehicle we tested: 30% PEG400/0.5% Tween80/5% propylene glycol (Solubility: 30mg/ml).
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