CYP3 选择性抑制剂 | 激活剂

目录号 产品名 产品描述 Selective / Pan IC50 / Ki
S2476 Itraconazole (R 51211)

Itraconazole是一种三唑类抗真菌药物,是CYP3A4的有效抑制剂,IC50为6.1 nM。

Selective CYP3A4, IC50: 6.1 nM
S2921 PF-4981517

PF-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。

Selective CYP3A4, IC50: 30 nM
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。

Selective CYP3A, IC50: 30 nM-285 nM
S6868 Alflutinib (AST2818) mesylate

Alflutinib is an inhibitor of EGFR that targets both EGFR activating mutations and T790M, thus leading to tumor growth inhibition.

Selective CYP3A4, EC50: 0.25 μM
S3766 Tanshinone IIA sulfonate sodium

Sodium tanshinone IIA sulfonate (STS) is a water-soluble derivative of tanshinone IIA isolated as the main pharmacologically active natural compound from a traditional Chinese herbal medicine, the dried root of Salvia miltiorrhiza Bunge known as Danshen. Sodium tanshinone IIA sulfonate (STS) is a potent negative allosteric modulator of the human purinergic receptor P2X7. Sodium tanshinone IIA sulfonate (STS) inhibits the activity of CYP3A4 and store-operated Ca2+ entry (SOCE)

Selective CYP3A4, IC50: 6.377 μM
S3874 Curcumenol

Curcumenol, a sesquiterpene isolated from Curcuma zedoaria, is known to possess a variety of health and medicinal values which includes neuroprotection, anti-inflammatory, anti-tumor and hepatoprotective activities. It inhibits NF-κB activation by suppressing the nuclear translocation of the NF-κB p65 subunit and blocking IκBα phosphorylation and degradation.

Selective CYP3A4, IC50: 12.6 μM
S9442 Bergaptol

Bergaptol (5-Hydroxypsoralen, 5-Hydroxyfuranocoumarin) is a natural furanocoumarin found in the essential oils of citrus including lemon and bergamot.Bergaptol is a potent inhibitors of debenzylation activity of CYP3A4 enzyme with an IC50 value of 24.92 μM.

Selective CYP3A4, IC50: 24.92 μM
S9299 Ginsenoside F1

Ginsenoside F1, a pharmaceutical component of ginseng, is known to have antiaging, antioxidant, anticancer, and keratinocyte protective effects. Ginsenoside F1 exhibits competitive inhibition of the activity of CYP3A4 with Ki values of 67.8 ± 16.2 μM. Ginsenoside F1 also exhibited a weaker inhibition of the activity of CYP2D6.

Selective CYP3A4, Ki: 67.8 μM
S9250 Isosilybin

Isosilybin (Silymarin, Silybin B, Isosilybinin, Q-100795) is a flavanolignan found in the extract of S. marianum fruits with antioxidant and anticancer activities. Isosilybin inhibits CYP3A4 induction with an IC50 of 74 μM.

Selective CYP3A4, IC50: 74 μM
S1185 Ritonavir (ABT-538)

Ritonavir是Cytochrome P450 3AHIV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 2B6UDP Glucuronosyltransferases

Selective
S2555 Clarithromycin

Clarithromycin 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。

Selective
S3227 5,7-Dimethoxyflavone

5,7-Dimethoxyflavone (5,7-DMF) is an inhibitor of cytochrome P450 (CYP) 3As that markedly decreases the expression of CYP3A11 and CYP3A25 in the liver. 5,7-Dimethoxyflavone (5,7-DMF) is also a potent Breast Cancer Resistance Protein (BCRP, ABCG2) inhibitor. 5,7-Dimethoxyflavone (5,7-DMF) is one of the major components of Kaempferia parviflora with anti-obesity, anti-inflammatory, and antineoplastic effects.

Selective
S1257 Posaconazole (SCH 56592)

Posaconazole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。

Selective
S2344 Piperine

Piperine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。

Selective
S4938 Cedrol

Cedrol, a natural occuring sesquiterpene alcohol, is a potent competitive inhibitor of CYP2B6-mediated bupropion hydroxylase with inhibition constant (Ki) value of 0.9 μM. It also inhibits CYP3A4-mediated midazolam hydroxylation with a Ki value of 3.4 μM while only weakly inhibits CYP2C8, CYP2C9, and CYP2C19 activities.

Pan CYP3A4, Ki: 3.4 μM
S2046 Pioglitazone HCl

Pioglitazone 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。

Pan CYP3A4, Ki: 11.8 μM
S3931 Ginsenoside Rd

Ginsenoside Rd (Panaxoside Rd, Sanchinoside Rd), a minor ginseng saponin, has several pharmacological activities such as immunosuppressive activity, anti-inflammatory activity, immunological adjuvant, anti-cancer activity and wound-healing activity. Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca2+ influx. Ginsenoside Rd inhibits CYP2D6, CYP

Pan CYP3A4, IC50: 81.7 μM