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26

抑制剂 & 化合物

3

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T7556	Fadrozole hydrochloride CGS 16949A,盐酸法倔唑	Aromatase	Endocrinology/Hormones
	Fadrozole hydrochloride (CGS 16949A) 是一种选择性的、有效，和非甾体类的芳香化酶抑制剂(IC50:6.4 nM)。
T25283	Cytochrome P450 2C9 Cyp2C9,Human cytochrome P450 2C9,Cytochrome P 450 2C9,S-Mephenytoin 4-hydroxylase
	Cytochrome P450 2C9 is a cytochrome P-450 subtype that possesses specificity for acidic xenobiotics. It oxidizes a wide range of important clinical drugs under the categories of nonsteroidal anti-inflammatory agents, anticoagulants, hypoglycemic agents, a
TP2238	Cytochrome P450 CYP1B1 (190-198) [Homo sapiens]	Others	Others
	Cytochrome c is a small heme protein found loosely associated with the inner membrane of the mitochondrion. Cytochromes c from certain eukaryotes, including plants and fungi but not higher animals, contains methylated lysine residues at specific positions
T117521	7-BFC 7-Benzyloxy-4-(trifluoromethyl)coumarin,Y040-0031	P450	Metabolism
	7-BFC (7-Benzyloxy-4-(trifluoromethyl)coumarin) 是一种香豆素类荧光底物，可作为细胞色素 P 450 的生物标记物，可用于研究 CYP 亚型和细胞色素 P 450 代谢。
T1597	Proadifen hydrochloride U-5446,RP-5171,SKF-525A,盐酸丙基解痉素	P450	Metabolism
	Proadifen hydrochloride (RP-5171) 是细胞色素 P450抑制剂，它的 IC50值为19μM。
T1378	Tegafur Fluorafur,替加氟,FT-207,NSC 148958,FT 207	Nucleoside Antimetabolite/Analog; DNA/RNA Synthesis	Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	Tegafur (FT 207) 是一种前药，在肝脏中被细胞色素 P-450 酶逐渐转化为氟尿嘧啶。它是抗代谢物氟尿嘧啶的同源物，具有抗肿瘤活性。
T27918	LY 43578 LY-43578,LY43578	P450; Aromatase	Endocrinology/Hormones; Metabolism
	LY 43578 是一种具有口服活性的芳香酶 (aromatase) 抑制剂。LY 43578 对大鼠肝微粒体 P-450依赖的 p-nitroanisole 的 O -去甲基化和 ethylmorphine 的 N -去甲基化有抑制作用，IC50 分别为 0.3 和 5 μΜ。LY 43578 可用于研究神经系统疾病和心血管疾病。
T0120	Voriconazole UK-109496,伏立康唑	Antifection; Antifungal	Microbiology/Virology
	Voriconazole (UK-109496) 是一种三唑类抗真菌剂，可抑制真菌麦角甾醇的生物合成。它特异性抑制由真菌细胞色素 P450 酶介导的 14-α-羊毛甾醇去甲基化作用
T7696	3-Cyano-7-ethoxycoumarin	Others	Others
	3-Cyano-7-ethoxycoumarin 是荧光色素 P-450底物，在酶切时获得蓝色荧光产物。
T6686	Sulconazole mononitrate Exelderm,Sulconazole Nitrate,RS 44872,硝酸硫康唑	Antibacterial; Antibiotic; Antifungal	Microbiology/Virology
	Sulconazole mononitrate (Exelderm) 是一种咪唑类广谱杀菌剂。它可研究皮肤真菌病，花斑糠疹病，皮肤念珠菌病。
T0922	Zoxazolamine NSC 24995,Contrazole,氯苯恶唑胺,苯并恶唑胺	Others	Others
	Zoxazolamine (NSC-24995) 是排尿酸和肌肉松弛剂，被广泛用于药物测试，可作为啮齿动物细胞色素 P-450 活性变化的方便指标。
T5952	Diniconazole 烯唑醇,Rac-diniconazole	Antibacterial	Microbiology/Virology
	Diniconazole (Rac-diniconazole) 是新型杀菌剂, 抑制由酵母细胞色素P-450催化的羊毛甾醇14α-脱甲基化。
T22229	Acid Yellow 36 Metanil Yellow,酸性黄36	Others	Others
	Acid Yellow 36 (Metanil Yellow) 是一种偶氮染料和 pH 指示剂，当 pH 值从 1.2 到 2.3 时，发生由红色到黄色的颜色转变。它是 P-450 特异性同工酶和胞浆酶的双功能诱导剂，可用于皮革、造纸和纺织工业。
T31815	Flumecinol Zyxorin
	Flumecinol is a hepatic enzyme (cytochrome P-450 monooxygenases) inducer.
T33110	M 79193 M79193,M-79193
	M 79193 induces total hepatic microsomal cytochrome P-450.
T25591	Lab 170250F Lab-170250F,Lab170250F
	Lab 170250F is a potent cytochrome P-450-obtusifoliol-14-demethylase inhibitor.
T34990	UK 39671
	UK 39671 is an inhibitor of cytochrome P-450(CAM) inhibitor.
T69553	p,p'-DDMS
	p,p'-DDMS is a water soluble and highly specific inhibitor of cytochrome P-450 omega-hydroxylase.
T69167	Buthiobate
	Buthiobate is a fungicide which inhibits lanosterol 14 alpha-demethylation catalyzed by a cytochrome P-450.
T78069	RPR132595A hydrochloride NPC hydrochloride	Drug Metabolite	Metabolism
	RPR132595A (NPC) hydrochloride，CPT-11的活性代谢产物，由细胞色素P-450 3A4 (CYP3A4) 催化产生，经尿液排出体外。
T19553	RPR132595A NPC	Others	Others
	RPR132595A is an active CPT-11 metabolite, it is generated by cytochrome P-450 3A4 (CYP3A4).
T78135	Nicotelline Nicotellin
	Nicotelline（Nicotellin）是一种与尼古丁相关的生物碱，作为人类cDNA表达的细胞色素P-450 2A6（CYP2A6）的弱抑制剂，不显著抑制该酶介导的香豆素7-羟基化反应，在300 μM浓度下效果更是如此。此外，Nicotelline还被用作烟草烟雾中颗粒物（PM）的示踪剂和生物标记物。
T36666	Dehydro Warfarin
	Dehydro warfarin is a metabolite of (±)-warfarin .1It is formed from (±)-warfarin by rat liver microsomes. 1.Kaminsky, L.S., Fasco, M.J., and Guengerich, F.P.Comparison of different forms of liver, kidney, and lung microsomal cytochrome P-450 by immunological inhibition of regio- and stereoselective metabolism of warfarinJ. Biol. Chem.254(19)9657-9662(1979)
T61259	Valganciclovir
	Valganciclovir 是ganciclovir 的原药，具有抗巨细胞病毒CMV 感染的活性。
T38269	Purfalcamine
	Purfalcamine is an orally active, selective Plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1) inhibitor with an IC50 of 17 nM and an EC50 of 230 nM. Purfalcamine has antimalarial activity and causes malaria parasites developmental arrest at the schizont stage[1][2]. Purfalcamine has low activity against Toxoplasma gondii calcium-dependent protein kinase 3 (TgCDPK3)[1]. Purfalcamine (225, 450 nM) has no effect on the parasitemia in the first 32 hours. After about 40 hours, paras...
T35463	(±)14(15)-EET (±)14,15-EET,(±)14,15-EpETrE,(±)14(15)-EET
	(±)14(15)-EET is a metabolite of arachidonic acid that is formed via epoxidation of arachidonic acid by cytochrome P450.[1],[2] It prevents increases in leukotriene B4, ICAM-1, and chemokine (C-C motif) ligand 1 (CCL2) induced by oxidized LDL in primary rat pulmonary artery endothelial cells (RPAECs) when used at a concentration of 1 μM.[3] (±)14(15)-EET induces dilation of preconstricted isolated canine coronary arterioles (EC50 = 0.2 pM).[4] It reduces myocardial infarct size as a percentage o...

化合物

Fadrozole hydrochloride

Cat.No: T7556

Synonym: CGS 16949A,盐酸法倔唑

Target: Aromatase

Cytochrome P450 2C9

Cat.No: T25283

Synonym: Cyp2C9,Human cytochrome P450 2C9,Cytochrome P 450 2C9,S-Mephenytoin 4-hydroxylase

Cytochrome P450 CYP1B1 (190-198) [Homo sapiens]

Cat.No: TP2238

Target: Others

Cat.No: T117521

Synonym: 7-Benzyloxy-4-(trifluoromethyl)coumarin,Y040-0031

Target: P450

Proadifen hydrochloride

Cat.No: T1597

Synonym: U-5446,RP-5171,SKF-525A,盐酸丙基解痉素

Target: P450

Cat.No: T1378

Synonym: Fluorafur,替加氟,FT-207,NSC 148958,FT 207

Target: Nucleoside Antimetabolite/Analog, DNA/RNA Synthesis

Cat.No: T27918

Synonym: LY-43578,LY43578

Target: P450, Aromatase

Cat.No: T0120

Synonym: UK-109496,伏立康唑

Target: Antifection, Antifungal

3-Cyano-7-ethoxycoumarin

Cat.No: T7696

Target: Others

Sulconazole mononitrate

Cat.No: T6686

Synonym: Exelderm,Sulconazole Nitrate,RS 44872,硝酸硫康唑

Target: Antibacterial, Antibiotic, Antifungal

Cat.No: T0922

Synonym: NSC 24995,Contrazole,氯苯恶唑胺,苯并恶唑胺

Target: Others

Cat.No: T5952

Synonym: 烯唑醇,Rac-diniconazole

Target: Antibacterial

Cat.No: T22229

Synonym: Metanil Yellow,酸性黄36

Target: Others

Cat.No: T31815

Synonym: Zyxorin

Cat.No: T33110

Synonym: M79193,M-79193

Cat.No: T25591

Synonym: Lab-170250F,Lab170250F

Cat.No: T34990

Cat.No: T69553

Cat.No: T69167

RPR132595A hydrochloride

Cat.No: T78069

Synonym: NPC hydrochloride

Target: Drug Metabolite

Cat.No: T19553

Synonym: NPC

Target: Others

Cat.No: T78135

Synonym: Nicotellin

Dehydro Warfarin

Cat.No: T36666

Cat.No: T61259

Cat.No: T38269

Cat.No: T35463

Synonym: (±)14,15-EET,(±)14,15-EpETrE,(±)14(15)-EET

Cat. No.	Product Name	Target	Signaling Pathways
TN1078	Seneciphylline 千里光菲灵碱,千里光非灵	P450; GST	Metabolism; oxidation-reduction
	Seneciphylline 是一种有毒的吡咯烷核生物碱，存在于千里光植物中。它显著增加了环氧水合酶和谷胱甘肽-S-转移酶的特性，但导致细胞色素 P-450 和相关单加氧酶特性的抑制。
T1011	Itraconazole 伊曲康唑,R51211	P450; Hedgehog/Smoothened; Antibiotic; Autophagy; Antifungal	Autophagy; GPCR/G Protein; Metabolism; Microbiology/Virology; Stem Cells
	Itraconazole (R51211) 是三唑类抗真菌药，也是口服活性的Hedgehog 信号通路拮抗剂，IC50约为 800 nM。它也是 oxysterol-binding protein 抑制剂。它抑制羊毛甾醇 14α-脱甲基酶，从而抑制羊毛甾醇向麦角固醇的氧化转化。它有抗癌和抗血管作用。
T40859	5-Hydroxy-8-methoxypsoralen 5-Hydroxyxanthotoxin,5-Hydroxy-8-methoxypsoralen
	5-Hydroxy-8-methoxypsoralen (5-Hydroxyxanthotoxin) is a metabolite derived from Xanthotoxin, which acts as a potent tricyclic furocoumarin suicide inhibitor of CYP (cytochrome P-450). It is employed as an agent for the treatment of psoriasis, eczema, vitiligo, and certain cutaneous Lymphomas, in combination with phototherapy involving exposure to sunlight.

天然产物

Cat.No: TN1078

Synonym: 千里光菲灵碱,千里光非灵

Target: P450, GST

Cat.No: T1011

Synonym: 伊曲康唑,R51211

Target: P450, Hedgehog/Smoothened, Antibiotic, Autophagy, Antifungal

5-Hydroxy-8-methoxypsoralen

Cat.No: T40859

Synonym: 5-Hydroxyxanthotoxin,5-Hydroxy-8-methoxypsoralen

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