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)
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
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
S3777 Gentiopicroside -1 mg/mL 71 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
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
S2401 Sodium Danshensu 2 mg/mL 7 mg/mL <1 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

特异性亚型抑制剂

产品目录 产品描述 文献引用 实验数据
S1123

Abiraterone

Abiraterone是一种有效CYP17抑制剂,无细胞试验中IC50为2 nM。

S1185

Ritonavir

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

S2246

Abiraterone Acetate

Abiraterone 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。

S1257

Posaconazole

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。

S1442

Voriconazole

Voriconazole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。

S5380New

7-Hydroxyflavone

7-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.

S5266New

Stiripentol

Stiripentol is a third-generation anti-epileptic drug that enhances GABAergic neurotransmission. It is an inhibitor of cytochrome P450.

S5529New

Galangin

Galangin, 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.

S5429New

Diallyl sulfide

Diallyl 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.

S4938New

Cedrol

Cedrol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。

S3777New

Gentiopicroside

Gentiopicroside (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.

S3673New

Sulfaphenazole

Sulfaphenazole 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).

S3660New

Uniconazole

Uniconazole 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.

S2187

Avasimibe

Avasimibe抑制ACATIC50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,

S1353

Ketoconazole

Ketoconazole能抑制cyclosporine oxidase(环孢素氧化酶)testosterone 6 beta-hydroxylase(睾丸素6β-羟化酶)IC50分别为0.19 mM和0.22 mM。

S2476

Itraconazole

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。

S1331

Fluconazole

Fluconazole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。

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。

S2803

Galeterone

Galeterone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。

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。

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。

S2496

Ozagrel

Ozagrel是一种有效的,选择性的血栓素A2合成酶抑制剂,IC50为4 nM。

S1739

Thiabendazole

Thiabendazole 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。

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。

S2067

Ozagrel HCl

Ozagrel 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。

S1952

Methoxsalen

Methoxsalen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。

S2526

Alizarin

Alizarin强效抑制P450亚型CYP1A1, CYP1A2和CYP1B1IC50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。

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。

S2043

Memantine HCl

Memantine HCl是一种CYP2B6CYP2D6抑制剂,作用于重组CYP2B6和CYP2D6,Ki分别为0.51 nM和94.9 μM。

S2380

Diosmetin

Diosmetin 是在Spearmint, Oregano, 和许多其他植物中发现的生物类黄酮。

S2262

Apigenin

Apigenin是一种有效的CYP2C9抑制剂,Ki为2 μM.。

S2268

Baicalein

Baicalein是CYP2C9和脯氨酰肽链内切酶抑制剂。

S2389

Naringin Dihydrochalcone

Naringin 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。

S2394

Naringenin

Naringenin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。

S2401

Sodium Danshensu

Sodium 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。

S2329

Naringin

Naringin 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。

S4221

Benzbromarone

Benzbromarone 是CYP2C9抑制剂,与CYP2C9 结合,Ki为19.3 nM。

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。

S1712

Deferasirox

Deferasirox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。

S4155

Chlorzoxazone

Chlorzoxazone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。

S4741

Danshensu

Danshensu(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。