P450 (e.g. CYP17)
信号通路图
研究领域
- 抑制剂选择性比较
- 溶解性比较
| 目录号 | 产品目录 | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | 酒精 | ||
| S1123 | Abiraterone | 0.02 mg/mL | 0.1 mg/mL | 0.2 mg/mL |
| S1185 | Ritonavir | <1 mg/mL | 100 mg/mL | 3 mg/mL |
| S2246 | Abiraterone Acetate | <1 mg/mL | <1 mg/mL | 28 mg/mL |
| S1257 | Posaconazole | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S1442 | Voriconazole | <1 mg/mL | 70 mg/mL | 20 mg/mL |
| S9257 | Acetylshikonin | -1 mg/mL | 2 mg/mL | -1 mg/mL |
| S9163 | Rhapontigenin | -1 mg/mL | 51 mg/mL | -1 mg/mL |
| S5380 | 7-Hydroxyflavone | -1 mg/mL | 47 mg/mL | -1 mg/mL |
| S5266 | Stiripentol | 13 mg/mL | 46 mg/mL | 46 mg/mL |
| S5529 | Galangin | <1 mg/mL | 54 mg/mL | 30 mg/mL |
| S4938 | Cedrol | -1 mg/mL | 44 mg/mL | -1 mg/mL |
| S2187 | Avasimibe | <1 mg/mL | 100 mg/mL | 8 mg/mL |
| S1353 | Ketoconazole | <1 mg/mL | 5 mg/mL | 7 mg/mL |
| S2476 | Itraconazole | <1 mg/mL | 7 mg/mL | <1 mg/mL |
| S1331 | Fluconazole | <1 mg/mL | 61 mg/mL | 61 mg/mL |
| S1195 | TAK-700 (Orteronel) | <1 mg/mL | 61 mg/mL | 8 mg/mL |
| S2803 | Galeterone | <1 mg/mL | 24 mg/mL | 40 mg/mL |
| S2555 | Clarithromycin | <1 mg/mL | 25 mg/mL | <1 mg/mL |
| S2900 | Cobicistat (GS-9350) | <1 mg/mL | 100 mg/mL | 100 mg/mL |
| S2496 | Ozagrel | <1 mg/mL | 46 mg/mL | <1 mg/mL |
| S1739 | Thiabendazole | <1 mg/mL | 40 mg/mL | 1 mg/mL |
| S2046 | Pioglitazone HCl | <1 mg/mL | 79 mg/mL | 4 mg/mL |
| S2067 | Ozagrel HCl | 52 mg/mL | 52 mg/mL | 6 mg/mL |
| S1952 | Methoxsalen | <1 mg/mL | 43 mg/mL | 5 mg/mL |
| S2526 | Alizarin | <1 mg/mL | 48 mg/mL | <1 mg/mL |
| S2921 | PF-4981517 | <1 mg/mL | 91 mg/mL | <1 mg/mL |
| S2043 | Memantine HCl | 30 mg/mL | 43 mg/mL | 43 mg/mL |
| S2380 | Diosmetin | <1 mg/mL | 60 mg/mL | <1 mg/mL |
| S2262 | Apigenin | <1 mg/mL | 54 mg/mL | <1 mg/mL |
| S2268 | Baicalein | <1 mg/mL | 54 mg/mL | <1 mg/mL |
| S2389 | Naringin Dihydrochalcone | <1 mg/mL | 100 mg/mL | 100 mg/mL |
| S2394 | Naringenin | <1 mg/mL | 54 mg/mL | 5 mg/mL |
| S3777 | Gentiopicroside | -1 mg/mL | 71 mg/mL | -1 mg/mL |
| S2401 | Sodium Danshensu | 2 mg/mL | 7 mg/mL | <1 mg/mL |
| S3673 | Sulfaphenazole | <1 mg/mL | 62 mg/mL | 62 mg/mL |
| S3660 | Uniconazole | <1 mg/mL | 58 mg/mL | 58 mg/mL |
| S2329 | Naringin | <1 mg/mL | 100 mg/mL | 2 mg/mL |
| S4221 | Benzbromarone | <1 mg/mL | 85 mg/mL | 9 mg/mL |
| S2344 | Piperine | <1 mg/mL | 57 mg/mL | 57 mg/mL |
| S1712 | Deferasirox | <1 mg/mL | 74 mg/mL | 2 mg/mL |
| S4155 | Chlorzoxazone | <1 mg/mL | 34 mg/mL | 34 mg/mL |
| S4741 | Danshensu | 23 mg/mL | <1 mg/mL | <1 mg/mL |
- P450 (e.g. CYP17)抑制剂（43）
- 新P450 (e.g. CYP17)产品
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1123 |
AbirateroneAbiraterone是一种有效CYP17抑制剂，无细胞试验中IC50为2 nM。 |
A. ZR75-1 (AR+, ER+) and B. MDA MB 231 (AR-, TNBC) cells were treated with either abiraterone or vehicle, then used as targets in a CTL assay using CEA-specific CD8+ T cells as effector cells at an E:T ratio of 30:1. Error bars indicate mean ± S.E.M. for quadruplicate measurements. Statistical analyses were done by Student's t-test, * = P < 0.01 vs. vehicle control. Data are representative of 2 independent experiments.
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| S1185 |
RitonavirRitonavir是Cytochrome P450 3A和HIV蛋白酶抑制剂，用于治疗HIV感染和AIDS。抑制Cytochrome P450 2D6, P-Glycoprotein，诱导Cytochrome P450 2C19, Cytochrome P450 1A2, Cytochrome P450 2C9, Cytochrome P450 2B6和UDP Glucuronosyltransferases。 |
(A) KMS11 and
(B) L363 cells were plated in 5mM glucose medium with ritonavir or DMSO (D) for 17 hours. Glucose consumption rates are normalized to untreated cells (not shown).
(C) KMS11 and (D) L363 cells were treated with ritonavir or DMSO for 72 hours. Relative viable cell numbers were determined by MTS assay and normalized to
untreated cells (not shown).
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| S2246 |
Abiraterone AcetateAbiraterone Acetate是Abiraterone的醋酸盐形式，是一种甾体类细胞色素CYP17抑制剂，无细胞试验中IC50为72 nM。 |
Concomitant Western blot analysis of ER and TFF1 assessed after 16 h treatment with E2 or abiraterone in the presence or absence of MG-132 (10 μM).
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| S1257 |
PosaconazolePosaconazole是CYP3A4的抑制剂，但不抑制其他CYP酶的活性；同时是sterol C14ɑ demethylase的抑制剂，IC50为0.25 μM。其平均的消除半衰期为15-35小时。 |
Comparative mean±SD plasma concentration versus time curves of 40mg/kg oral posaconazole (PSZ) administrated in normolipidemic (NL), intermediate hyperlipidemic (IHL) or
extreme hyperlipidemic (HL) rat groups. An insert showing a clear snap of the plasma concentrations for the first 7 h.
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| S1442 |
VoriconazoleVoriconazole是一种三唑类抗真菌药物，用于治疗严重的侵入性真菌感染。 |
Voriconazole increases the osteogenic activity of human osteoblasts in vitro. Osteoblasts were exposed to voriconazole (VCZ) or fluconazole (FCZ) at 15 or 200 μg/ml in osteoinductive medium (OS+) for up to 7 days. As a positive control, cells were also exposed to sodium fluoride (NaF) at 10 μM in nonosteoinductive medium (OS−). Osteoblastic differentiation was evaluated by measuring alkaline phosphatase (ALP) activity (A) and staining for calcium deposition with alazarin red S stain (B and C); calcium deposition was quantified by measuring the absorbance (A415) of extracted alazarin red S (B) and was assessed by the light microscopic appearance (white arrows) of stained osteoblast cultures (C). Values represent the means ± SD. *, P < 0.05, compared to osteoblasts grown under osteogenic conditions without treatment. |
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| S9257New |
AcetylshikoninAcetylshikonin is a biologically active compound with anti-cancer and anti-inflammatory activity, which is isolated from the roots of Lithospermum erythrorhizoma. It is a novel general P450 inhibitor with IC50 values of 1.4-4.0 μM for all tested P450s. |
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| S9163New |
RhapontigeninRhapontigenin, produced from rhapontin isolated from a methanol extract of Rheum undulatum roots by enzymatic transformation, is a selective inactivator of cytochrome P450 1A1 (IC50 = 400 nM). |
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| S5380New |
7-Hydroxyflavone7-Hydroxyflavone is a potent inhibitor of CYP1A1 with a Ki value of 0.015 μM and exhibits 6-fold greater selectivity for CYP1A1 over CYP1A2. It also has excellent antioxidant properties and great potential to be applied as medicines. |
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| S5266New |
StiripentolStiripentol is a third-generation anti-epileptic drug that enhances GABAergic neurotransmission. It is an inhibitor of cytochrome P450. |
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| S5529New |
GalanginGalangin, a naturally occuring flavonoid found in herbs, is a well-known antioxidant and also an inhibitor of CYP1A1 activity and an agonist/antagonist of the aryl hydrocarbon receptor. |
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| S5429New |
Diallyl sulfideDiallyl sulfide, a thioether found naturally in garlic, is a selective inhibitor and also a substrate of CYP2E1 with an IC50 of 17.3 μM. It has protective effects against alcohol- and acetaminophen-induced hepatotoxicity in many studies. |
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| S4938New |
CedrolCedrol是一种天然存在的倍半萜烯醇，是有效的、竞争性的抑制剂，抑制CYP2B6介导的安非他酮羟化酶(bupropion hydroxylase)，Ki值为0.9 μM。它还能抑制CYP3A4介导的咪达唑仑羟基化，Ki为3.4 μM。对CYP2C8, CYP2C9和CYP2C19的活性仅有微弱的抑制作用。 |
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| S2187 |
AvasimibeAvasimibe抑制ACAT，IC50为3.3 μM，也抑制人P450同工酶CYP2C9， CYP1A2和CYP2C19，IC50分别为2.9 μM， 13.9 μM和26.5 μM， |
a, b, Melanoma-bearing mice were treated with avasimibe (Ava) or DMSO control (5 times) (control, n=9; avasimibe, n=8). c-e, STORM analysis of TCR clustering of tumour-infiltrating CD8+ T cells. c, Representative images. d, Ripley’s K-function analysis of TCR molecules. e, The r value at the maximal L(r)-r value of Ripley’s K-function curves (control, n=100; avasimibe, n=85). f, g, A combined therapy (avasimibe and anti-PD-1) or monotherapies (avasimibe or anti-PD-1) in treating melanoma (n=10). Avasimibe, 5 times; anti-PD-1, 4 times. h, i, Cytokine/granule productions of PD-1hi and PD-1lo tumour-infiltrating CD8+ T cells (control, n=12; avasimibe, n=11). |
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| S1353 |
KetoconazoleKetoconazole能抑制cyclosporine oxidase（环孢素氧化酶）和testosterone 6 beta-hydroxylase（睾丸素6β-羟化酶），IC50分别为0.19 mM和0.22 mM。 |
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| S2476 |
ItraconazoleItraconazole是一种三唑类抗真菌药物，是CYP3A4的有效抑制剂，IC50为6.1 nM。 |
Resistance to itraconazole in MA cells. The parental SUM149-Luc cell line and MA1 cells were treated in parallel with 1 mM itraconazole for 9 days (which killed most of the cells in the parental cell line) and were allowed to recover and grow in a drug-free medium for 5 days before being stained. Since itraconazole was ineffective in killing MA1 cells, the cells grew into a continuous monolayer rather than colonies. |
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| S1331 |
FluconazoleFluconazole是一种羊毛甾醇14 alpha去甲基化酶 抑制剂，抑制了麦角固醇的形成，用于治疗和预防浅表性和全身性真菌感染。 |
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| S1195 |
TAK-700 (Orteronel)TAK-700 (Orteronel)是一种有效的，高度选择性的，人17，20-lyase抑制剂，IC50为38 nM，比作用于其他CYPs(例如11-羟化酶和CYP3A4)选择性高1000倍以上。Phase 3。 |
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| S2803 |
GaleteroneGaleterone是一种选择性CYP17抑制剂，也是androgen receptor (AR)（雄激素受体）拮抗剂，IC50分别为300 nM和384 nM，也有效抑制人类前列腺肿瘤生长。Phase 2。 |
C. Impact of CYP17A1 inhibitors on genes involved in androgen biosynthesis. H295R cells were treated with control (DMSO) or 1 μM orteronel and galeterone for 72 h and then RNA was isolated and transcribed to cDNA. Results of qRT-PCR validation of HSD3B2, CYP17A1 and AKR1C3 genes relative to the housekeeping gene cyclophilin A. Expression of the genes was analyzed by SYBR Green real-time PCR. Analysis of relative gene expression was determined by the 2−ΔΔCt method. *p < 0.05. |
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| S2555 |
ClarithromycinClarithromycin 是一种大环内酯类抗生素，是CYP3A4抑制剂，用于治疗许多细菌感染。 |
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| S2900 |
Cobicistat (GS-9350)Cobicistat (GS-9350)是一种有效的CYP3A选择性抑制剂，IC50为30 - 285 nM。 |
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| S2496 |
OzagrelOzagrel是一种有效的，选择性的血栓素A2合成酶抑制剂，IC50为4 nM。 |
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| S1739 |
ThiabendazoleThiabendazole 抑制线粒体蠕虫特异性酶，延胡索酸还原酶，具有驱虫药的性能。是一种有效的CYP1A2的抑制剂。 |
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| S2046 |
Pioglitazone HClPioglitazone HCl是Pioglitazone的盐酸盐形式，是细胞色素P450 (CYP)2C8和CYP3A4酶抑制剂，作用于CYP2C8， CYP3A4和CYP2C9， Ki分别为1.7 μM， 11.8 μM和32.1 μM。 |
Primary hepatocytes were treated with or without 20μM Wy14643/Pioglitazone/Rosiglitazone for 24h followed by stimulation with or without 1μg/ml recombinant human FGF21 for 15min. FGF21 signaling was analyzed by phosphorylation of ERK1/2 and FRS2 examination. |
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| S2067 |
Ozagrel HClOzagrel HCl是选择性血栓素A2合成酶抑制剂，其在兔子血小板中IC50为11 nM, 用作改善手术后脑血管收缩，以及伴随的脑梗塞。 |
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| S1952 |
MethoxsalenMethoxsalen是在一些植物中发现的天然存在的呋喃香豆素化合物，包括补骨脂，用于治疗牛皮癣，湿疹，白癜风及一些暴露在阳光下的皮肤淋巴瘤。是CYP2A5/6抑制剂。 |
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| S2526 |
AlizarinAlizarin强效抑制P450亚型CYP1A1， CYP1A2和CYP1B1，IC50分别为6.2 μM， 10.0 μM and 2.7 μM，微弱抑制CYP2A6和CYP2E1，对CYP2C19，对CYP3A4和CYP3A5没有抑制作用。 |
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| S2921 |
PF-4981517PF-4981517是一种有效的，选择性的CYP3A4(P450)抑制剂，IC50为0.03 μM，比作用于CYP3A5和CYP3A7选择性高500倍以上。 |
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| S2043 |
Memantine HClMemantine HCl是一种CYP2B6和CYP2D6抑制剂，作用于重组CYP2B6和CYP2D6，Ki分别为0.51 nM和94.9 μM。 |
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| S2380 |
DiosmetinDiosmetin 是在Spearmint, Oregano, 和许多其他植物中发现的生物类黄酮。 |
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| S2262 |
ApigeninApigenin是一种有效的CYP2C9抑制剂，Ki为2 μM.。 |
The effects of apigenin and GLUT-1 AS-ODNs on xenograft apoptosis (the second experiment), observed an under optical microscope (magnification, ×400), and the percentage of apoptotic cells in 100 cells per field was counted and used to calculate the mean apoptosis index (AI). AI, apoptotic index.
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| S2268 |
BaicaleinBaicalein是CYP2C9和脯氨酰肽链内切酶抑制剂。 |
Baicalein suppresses the viability of DU 145 and PC-3 cells. b DU145 cells and c PC-3 cells were treated with different concentrations of baicalein for 24, 48, and 72 h. Baicalein significantly inhibited the viability of both cell lines in a dose-and time-dependent manner. The results are presented as the means ± SD of three independent experiments and the corresponding standard error. *P<0.05; **P<0.01. |
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| S2389 |
Naringin DihydrochalconeNaringin Dihydrochalcone 是一种新型甜味剂，是来自柚皮苷的一种人工甜味剂。也是一种CYP enzymes的抑制剂。 |
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| S2394 |
NaringeninNaringenin是来自于食用植物的一种天然的主要黄酮类化合物，有益人体健康，具有生物活性，是一种抗氧化剂，自由基清除剂，抗炎，碳水化合物代谢启动子及免疫系统的调制剂。 |
(d) Antiviral activity of SZA on assembly and release. Huh7 cells were electroporated with JFH-1 RNA of HCV, followed by 4 h treatment of the indicated concentrations of SZA. At 48 h after electroporation, cells were subjected to three cycles of freeze and thaw to test the intracellular viral infectivity; supernatants of the electroporated cells were collected for the detection of extracellular viral infectivity. 100 μM naringenin was introduced as a positive control. Results are shown as relative HCV infectivity compared to DMSO treated group. Data shown as mean ± SD of three independent experiments.
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| S3777 |
GentiopicrosideGentiopicroside (GE), a naturally occurring iridoid glycoside, inhibits CYP2A6 and CYP2E1 with IC50 values of 21.8μg/ml and 594μg/ml, respectively in human liver microsomes, and dose not inhibit CYP2C9, CYP2D6, CYP1A2 or CYP3A4 activities. |
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| S2401 |
Sodium DanshensuSodium Danshensu是丹参素的单钠盐，是从Salvia miltiorrhiza Bge中分离的天然酚酸，是咖啡酸衍生物。 |
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| S3673 |
SulfaphenazoleSulfaphenazole is an inhibitor of CYP2C9 with Ki value of 0.3 μM and demonstrates at least 100-fold selectivity over other CYP450 isoforms (Ki values of 63 and 29 μM for CYP2C8 and CYP2C18, respectively, and no activity at CYP1A1, CYP1A2, CYP3A4, CYP2C19). |
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| S3660 |
UniconazoleUniconazole is a plant growth regulator that functions by inhibiting cytochrome P450 707As (Ki = 68 nM), a family of enzymes that catabolize ABA. It suppress gibberellin and sterol biosynthesis. |
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| S2329 |
NaringinNaringin 是一种黄酮苷，是葡萄柚中的主要的类黄酮，具有柚子汁的苦味。具有抗氧化，降血脂，抗肿瘤活性，并且对cytochrome P450有抑制作用。 |
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| S4221 |
BenzbromaroneBenzbromarone 是CYP2C9抑制剂，与CYP2C9 结合，Ki为19.3 nM。 |
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| S2344 |
PiperinePiperine是一种生物碱，是造成黑胡椒和长胡椒辛辣的原因，也用于一些传统医学领域，且作为杀虫剂。 |
Piperine attenuates inflammation in the substantia nigra (SN) of the MPTP-treated brains. (A) Iba-1-immunostaining was performed on brain sections for microglia. Piperine alleviated microglia activating caused by MPTP. (B) Brain tissue was stained with the anti-interleukin-1β (IL-1β) antibody in the SN. MPTP notably increased the expression of IL-1β in the SN of the mice and the increase was partly blocked by piperine. (C) Western blot analysis of IL-1β expression in the SN. (D) Densitometric analysis of western blot analyses of IL-1β. Densitometry was measured by Quantity One 1-D analyze software (Universal Hood II; Bio-Rad Laboratories, Hercules, CA, USA). Values are presented as mean ± standard deviation, *P<0.05, compared to MPTP.
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| S1712 |
DeferasiroxDeferasirox是一种铁螯合剂，是cytochrome P450 3A4诱导剂，Cytochrome P450 2C8的抑制剂，Cytochrome P450 1A2抑制剂。 |
U2OS cells were cultured with FAC for 24 hours, washed, followed by chelation with 2 chelators (DFO, DFX) -/+ lysosomal protease inhibitors (E-64d and PepstatinA) and analyzed as in panel A. DFX: Deferasirox. |
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| S4155 |
ChlorzoxazoneChlorzoxazone是一种肌肉松弛的药物，作为人体肝脏细胞色素P-450IIE1的探针。 |
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| S4741 |
DanshensuDanshensu(丹参素)，是一种传统中药中的中草药，具有潜在的抗肿瘤和抗血管生成的效果。 |
