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32

抑制剂 & 化合物

1

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Cat. No.	Product Name	Target	Signaling Pathways
T11991	Mefentrifluconazole	P450; Antifungal	Metabolism; Microbiology/Virology
	Mefentrifluconazole 是一种有效的、选择性的和具有口服活性的真菌 CYP51 (Kd= 0.5 nM) 抑制剂，但对人芳香酶的抑制活性较低，IC50值为0.92 μM。它是一种新型唑类衍生物，用作农用广谱抗真菌剂。
T4190	Ticlopidine PCR 5332,Ticlid,噻氯匹定	ATPase; Adiponectin receptor	GPCR/G Protein; Membrane transporter/Ion channel
	Ticlopidine (PCR 5332) 是抗血栓前药。它是CYP2C19人肝细胞色素的抑制剂，抑制 CYP2C9 及 CYP3A4。他是变构CD39的非竞争性抑制剂，能够阻断 NTPDase 同工酶，对NTPDase2和NTPDase3的IC50分别为 170 µM 和 149 µM。
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。
T14983	Clomethiazole Distraneurin,Chlormethiazole,氯美噻唑,5-(2-CHLOROETHYL)-4-METHYLTHIAZOLE	P450; GABA Receptor	Membrane transporter/Ion channel; Metabolism; Neuroscience
	Clomethiazole (Distraneurin) 是口服GABAA 激动剂，可抑制人肝微粒体中的细胞色素 P450 异构体，CYP2A6 和 CYP2E1。它有抗惊厥作用，具有治疗惊厥性癫痫持续状态的潜力。
T67916	CYP4A11/CYP4F2-IN-2	P450	Metabolism
	CYP4A11/CYP4F2-IN-2 是一种有效的和具有口服活性的细胞色素 P450 (CYP) 4A11 和 CYP4F2 的双重抑制剂，IC50 值分别为 140 nM 和 40 nM。CYP4A11/CYP4F2-IN-2可从肝脏和肾脏中提取，具有治疗肾脏疾病的潜力。
T67791	BMS-903452	GPR	Endocrinology/Hormones; GPCR/G Protein
	BMS-903452是一种有效的、具有选择性的 GPR119激动剂，EC50为14 nM。BMS-903452可用于治疗急性和慢性啮齿动物糖尿病。GPR119主要在胰腺 b 细胞和胃肠道肠内分泌细胞中表达，对9种不同的细胞色素 P450酶没有显著的抑制作用(IC50 > 40 μM)，不激活 PXR (EC50>50 μM)，并且对肝脏(HEPG2)细胞系没有毒性。
T37149	Carbamazepine 10,11-epoxide	Others	Others
	Carbamazepine 10,11-epoxide 是抗惊厥药卡马西平 (carbamazepine) 的活性代谢物。它由卡马西平通过微粒体中的细胞色素 P450 (CYP) 同种型 CYP3A4 和 CYP2C8 形成，微粒体分别由表达 CYP3A4 或 CYP2C8 的 HepG2 细胞制备。它对小鼠电击诱发的癫痫发作具有抗惊厥活性。
T12280	O-Desmethyl Midostaurin CGP62221,O-Desmethyl PKC412	Others	Others
	O-Desmethyl Midostaurin is the active Midostaurin metabolite via cytochrome P450 liver enzyme metabolism.
T11584	Hydroxy desmethyl Bosentan Ro 64-1056	Others	Others
	Hydroxy desmethyl Bosentan (Ro 64-105) is a Bosentan metabolism produced by the cytochrome P450 enzymes CYP2C9 and CYP3A4 in the liver.
T24043	Erythromycin glutamate
	Erythromycin glutamate is a macrolide bacteriostatic antibiotic. This antibiotic is metabolized through the liver and inhibits cytochrome enzyme P450A 3A41.
T37430	Mirtazapine N-oxide
	Mirtazapine N-oxide is a metabolite of mirtazapine.1It is formed from mirtazapine by the cytochrome P450 (CYP) isoforms CYP1A2 and CYP3A4 in human liver microsomes.
T35715	N-desmethyl Eletriptan
	N-desmethyl Eletriptan is a metabolite of eletriptan .1It is formed from eletriptan primarily by the cytochrome P450 (CYP) isoform CYP3A4 in human liver microsomes. 1.Evans, D.C., O’Connor, D., Lake, B.G., et al.Eletriptan metabolism by human hepatic CYP450 enzymes and transport by human P-glycoproteinDrug Metab. Dispos.31(7)861-869(2003)
T36237	5-hydroxy Propranolol
	5-hydroxy Propranolol is a metabolite of propranolol , a β-adrenergic receptor antagonist. Propranolol is primarily metabolized in the liver, with cytochrome P450 isoform 2D6 directing ring hydroxylation and the generation of 5-hydroxy propranolol and related metabolites.
T35641	trans-hydroxy Glimepiride
	trans-hydroxy Glimepiride is an active metabolite of the sulfonylurea glimepiride .1It is formed from glimepiride primarily in the liver by the cytochrome P450 (CYP) isoform CYP2C9. 1.Langtry, H.D., and Balfour, J.A.Glimepiride. A review of its use in the management of type 2 diabetes mellitusDrugs55(4)563-584(1998)
T19360	Hydroxy bosentan Ro 48-5033	Others	Others
	Hydroxy bosentan (Ro 48-5033) is a primary metabolite of Bosentan (BOS) metabolized by the cytochrome P450 system in the liver. Hydroxy bosentan assists BOS pharmacologically, retaining 10%-20% activities.
T37454	C16 dihydro Ceramide (d18:0/16:0) Ceramide (d18:0/16:0),Cer(d18:0/16:0),N-hexadecanoyl-D-erythro-Dihydrosphingosine,N-Palmitoyl Sphinganine
	C16 dihydro Ceramide is a bioactive sphingolipid and precursor in the de novo synthesis of C16 ceramide (d18:0/16:0) that lacks the 4,5-trans double bond.[1] C16 dihydro Ceramide (0-46 nM) inhibits C16 ceramide-induced membrane permeabilization, measured as cytochrome C oxidation, in rat liver mitochondria in a concentration-dependent manner. It also inhibits C16 ceramide-induced channel formation in liposomes. C16 dihydro ceramide is biologically inactive as a single agent, lacking the ability ...
T36920	16α-hydroxy Dehydroepiandrosterone
	16α-hydroxy Dehydroepiandrosterone is a metabolite of the endogenous steroid hormone dehydroepiandrosterone .116α-hydroxy Dehydroepiandrosterone is formed from dehydroepiandrosteronevia16-hydroxylation by the cytochrome P450 (CYP) isoforms CYP3A4 and CYP3A5 in adult human liver microsomes, as well as by fetal recombinant CYP3A7. It is a precursor to fetal estrogens, including estriol .2 1.Miller, K.K.M., Cai, J., Ripp, S.L., et al.Stereo- and regioselectivity account for the diversity of dehydro...
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)
T36840	(R)-Omeprazole (sodium salt)
	(R)-Omeprazole is the inactive isomer of omeprazole , a gastric proton-pump inhibitor. A stereoselective hydroxylation of (R)-omeprazole is mediated primarily by cytochrome P450 (CYP) 2C19, whereas CYP3A4 favors sulfoxidation of the active (S)-enantiomer . (R)-Omeprazole has been shown to act as a reversible direct-acting and metabolism-dependent inhibitor of CYP2C19 in pooled human liver microsomes (IC50 = 8.1 μM).
T37229	(±)8,9-DiHETE
	(±)8,9-DiHETE is a major metabolite of the 20:5 ω-3 fatty acid eicosapentaenoic acid .[1] It is produced in rat liver microsomes, but not renal microsomes, by the generation of the unstable intermediate 8,9-epoxy eicosatetraenoic acid from EPA by cytochrome P450 monooxygenases. Dietary EPA supplementation in humans results in substantial urinary excretion of vicinal diols, including 8,9, 11,12, and 14,15 forms.[2]
T73762	11,12-DiHETrE
	11,12-DiHETrE，一种细胞色素P450 (P450) 类二十烷素内源性代谢产物，用于早产研究，并可作为区分NAFL(非酒精性脂肪肝)与NASH(非酒精性脂肪性肝炎)的生物标志物。
T69758	Flutamide-d7
	Flutamide-d7 is intended for use as an internal standard for the quantification of flutamide by GC- or LC-MS. Flutamide is an androgen receptor antagonist and prodrug form of 2-hydroxy flutamide. Flutamide is converted to 2-hydroxy flutamide by the cytochrome P450 (CYP) isoform CYP1A2 in human liver microsomes. It is cytotoxic to PC3 and LNCaP prostate cancer cells with IC50 values of 98.8 and 81.8 µM, respectively. Flutamide (50 mg/kg per day) reduces tumor growth in a PC-82 mouse xenograft mo...
T36681	Sorafenib N-oxide
	Sorafenib N-oxide is an active metabolite of sorafenib , an inhibitor of Raf-1, B-RAF, and receptor tyrosine kinases. Sorafenib N-oxide inhibits FLT3 that contains the internal tandem duplication mutation (FLT3-ITD; Kd = 70 nM) and inhibits proliferation of MV4-11 acute myeloid leukemia (AML) cells expressing FLT3-ITD (IC50 = 25.8 nM). It is selective for AML cell lines containing FLT3-ITD over lines containing wild-type FLT3 (IC50s = 3.9-13.3 μM). Sorafenib N-oxide is also a linear-mixed inhibi...
T35997	22-HDHA
	22-HDHA is an oxidation product of docosahexaenoic acid . In vitro, it is formed upon incubation of rat liver microsomes with DHA and NADPH and also by the human cytochrome P450 (CYP) isoform CYP4F3B in BTI-TN-5B1-4 microsomes. Serum levels of 22-HDHA increase following dietary DHA supplementation in humans.
T20765	Atorvastatin 阿托伐他汀,阿伐他汀	HMG-CoA Reductase; Autophagy	Autophagy; Metabolism
	Atorvastatin 是一种具有口服活性的 HMG-CoA 还原酶抑制剂，通过激活肝细胞色素p450加快代谢，具有有效降低血脂的能力。Atorvastatin 以 IC50 值分别为 0.39 μM 和 2.39 μM 来抑制人 SV-SMC 细胞的增殖和侵袭。Atorvastatin 与氯吡格雷同时服用两种可能会导致患者血栓事件增加。
T36074	S-NEPC
	Cytochrome P450 metabolites of arachidonic acid, such as 11(12)-EpETrE and 14(15)-EpETrE have been identified as endothelium derived hyperpolarizing factors with vasodilator activity. Soluble epoxide hydrolase (sEH) catalyzes the conversion of EpETrEs to the corresponding DiHETrEs thereby diminishing their activity. Inhibitors of sEH may therefore have clinical utility for treating hypertension and systemic inflammation. S-NEPC is a colorimetric substrate used to measure sEH activity. It also is...
T70661	Azalanstat mesylate
	Azalanstat is an anti-obesity drug acting as a lanosterol 14α-demethylase inhibitor. Azalanstat has been shown to inhibit cholesterol synthesis in HepG2 cells, human fibroblasts, hamster hepatocytes and hamster liver, by inhibiting the cytochrome P450 enzyme lanosterol 14 alpha-demethylase. When administered orally to hamsters fed regular chow, RS-21607 (50 mg/kg/day) lowered serum cholesterol in a dose-dependent manner (ED50 = 62 mg/kg) in a period of 1 week. It preferentially lowered low densi...
T70660	Azalanstat HCl
	Azalanstat is an anti-obesity drug acting as a lanosterol 14α-demethylase inhibitor. Azalanstat has been shown to inhibit cholesterol synthesis in HepG2 cells, human fibroblasts, hamster hepatocytes and hamster liver, by inhibiting the cytochrome P450 enzyme lanosterol 14 alpha-demethylase. When administered orally to hamsters fed regular chow, RS-21607 (50 mg/kg/day) lowered serum cholesterol in a dose-dependent manner (ED50 = 62 mg/kg) in a period of 1 week. It preferentially lowered low densi...
T13460	(+)-Cevimeline hydrochloride hemihydrate (+)-AF102B hydrochloride hemihydrate,(+)-SNI-2011	Others	Others
	(+)-Cevimeline hydrochloride hemihydrate ((+)-SNI-2011) 是一种有效的 mAChR 激动剂。
T13421	(-)-Cevimeline hydrochloride hemihydrate (-)-SNI-2011,(-)-AF102B hydrochloride hemihydrate	ALK	Angiogenesis; Tyrosine Kinase/Adaptors
	(-)-Cevimeline hydrochloride hemihydrate ((-)-SNI-2011) 是一种新型mAChR 激动剂，是一种治疗干燥综合征口干症的候选治疗药物。
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...
T35520	Aflatoxin G1-13C17 Aflatoxin G1-13C17
	Aflatoxin G1-13C17is intended for use as an internal standard for the quantification of aflatoxin G1by GC- or LC-MS. Aflatoxin G1is a mycotoxin that has been found inA. terricola.1In vivo, aflatoxin G1is lethal to ducklings (LD50= 1.18 mg/kg).2It induces hepatocellular carcinoma tumor formation and lethality in rats when administered at doses of 1.4 and 3 mg/animal, respectively. Aflatoxin G1also inhibits liver and kidney succinate dehydrogenase and fumarase, as well as kidney cytochrome oxidase...

化合物

Mefentrifluconazole

Cat.No: T11991

Target: P450, Antifungal

Cat.No: T4190

Synonym: PCR 5332,Ticlid,噻氯匹定

Target: ATPase, Adiponectin receptor

Cat.No: T1378

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

Target: Nucleoside Antimetabolite/Analog, DNA/RNA Synthesis

Cat.No: T14983

Synonym: Distraneurin,Chlormethiazole,氯美噻唑,5-(2-CHLOROETHYL)-4-METHYLTHIAZOLE

Target: P450, GABA Receptor

CYP4A11/CYP4F2-IN-2

Cat.No: T67916

Target: P450

Cat.No: T67791

Target: GPR

Carbamazepine 10,11-epoxide

Cat.No: T37149

Target: Others

O-Desmethyl Midostaurin

Cat.No: T12280

Synonym: CGP62221,O-Desmethyl PKC412

Target: Others

Hydroxy desmethyl Bosentan

Cat.No: T11584

Synonym: Ro 64-1056

Target: Others

Erythromycin glutamate

Cat.No: T24043

Mirtazapine N-oxide

Cat.No: T37430

N-desmethyl Eletriptan

Cat.No: T35715

5-hydroxy Propranolol

Cat.No: T36237

trans-hydroxy Glimepiride

Cat.No: T35641

Hydroxy bosentan

Cat.No: T19360

Synonym: Ro 48-5033

Target: Others

C16 dihydro Ceramide (d18:0/16:0)

Cat.No: T37454

Synonym: Ceramide (d18:0/16:0),Cer(d18:0/16:0),N-hexadecanoyl-D-erythro-Dihydrosphingosine,N-Palmitoyl Sphinganine

16α-hydroxy Dehydroepiandrosterone

Cat.No: T36920

Dehydro Warfarin

Cat.No: T36666

(R)-Omeprazole (sodium salt)

Cat.No: T36840

Cat.No: T37229

Cat.No: T73762

Cat.No: T69758

Sorafenib N-oxide

Cat.No: T36681

Cat.No: T35997

Cat.No: T20765

Synonym: 阿托伐他汀,阿伐他汀

Target: HMG-CoA Reductase, Autophagy

Cat.No: T36074

Azalanstat mesylate

Cat.No: T70661

Cat.No: T70660

(+)-Cevimeline hydrochloride hemihydrate

Cat.No: T13460

Synonym: (+)-AF102B hydrochloride hemihydrate,(+)-SNI-2011

Target: Others

(-)-Cevimeline hydrochloride hemihydrate

Cat.No: T13421

Synonym: (-)-SNI-2011,(-)-AF102B hydrochloride hemihydrate

Target: ALK

Cat.No: T35463

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

Aflatoxin G1-13C17

Cat.No: T35520

Synonym: Aflatoxin G1-13C17

Cat. No.	Product Name	Target	Signaling Pathways
T37810	6',7'-Epoxybergamottin
	6'7'-Epoxybergamottin is a furanocoumarin found in grapefruit. It is a potent inhibitor of the cytochrome P450 (CYP) isoform CYP3A4 with an IC50 value of 0.30 ppm in a cell-free assay, 0.33 μM in HL7 human liver cells, and 0.22 μM in S9 human intestine cells. It has been studied in the context of drug interactions with grapefruit constituents. It is found in grapefruit juice at concentrations of 0.1-7.4 μM and inhibits the transport of talinolol , a permeability glycoprotein (P-gp/ABCB1) transpo...

天然产物

6',7'-Epoxybergamottin

Cat.No: T37810

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