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17

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T12146	N-Desmethyl-Apalutamide N-Desmethyl Apalutamide,N-去甲基阿帕鲁胺杂质	P450; Androgen Receptor	Endocrinology/Hormones; Metabolism
	N-Desmethyl-Apalutamide 是一种 Apalutamide 的活性代谢产物，主要由 CYP2C8 和 CYP3A4 介导形成。它是一种低活性的雄激素受体拮抗剂，其作用力是 Apalutamide 活性的三分之一。它是中等至强的CYP3A4和CYP2B6诱导剂，并具有优异的血浆蛋白结合浓度。
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。
T4567	Sulfaphenazole Plisulfan,Raziosulfa,Depocid,磺胺苯吡唑,Depotsulfonamide	P450; Antibacterial	Metabolism; Microbiology/Virology
	Sulfaphenazole (Plisulfan) 是一种 CYP2C9的特异性抑制剂，抑制 CYP2C9介导的亚油酸动脉粥样硬化和促炎症效应，增加 AP-1的氧化应激和激活。
T41291	MS-PPOH	P450	Metabolism
	MS-PPOH 是一种有效的选择性细胞色素 P450 (CYP) 环氧化酶抑制剂。MS-PPOH 抑制 CYP2C8 和 CYP2C9，IC50 分别为 15 和 11 µM。
T1149	Fenofibrate Procetofen,非诺贝特,Lipanthyl,Lipantil	P450; PPAR; Autophagy	Autophagy; DNA Damage/DNA Repair; Metabolism
	Fenofibrate (Lipanthyl) 是一种选择性PPARα激动剂，EC50为 30 μM。它是一种合成的苯氧基异丁酸衍生物和前药，具有抗高血脂活性。它抑制细胞色素 P450 亚型, 对CYP2C19、CYP2B6、CYP2C9、CYP2C8和CYP3A4的IC50分别为 0.2、0.7、9.7、4.8 和 142.1 μM。
T13497	3'-Hydroxy Repaglinide	Others	Others
	3'-Hydroxy Repaglinide is a main CYP2C8 metabolite of Repaglinide. Repaglinide is a carbamoylmethyl benzoic acid derivative and used as the treatment of type II diabetes.
T11387	Gemfibrozil 1-O-β-glucuronide	Others	Others
	Gemfibrozil 1-O-β-Glucuronide, a metabolite of Gemfibrozil , is a potent and competitive P450 (CYP) isoform CYP2C8 inhibitor with an IC50 of 4.07 μM.
T67936	BAY-0069	PPAR	DNA Damage/DNA Repair; Metabolism
	BAY-0069 是一种 PPARγ 反向激活剂，具有有效性和选择性，对人 PPARγ 和鼠 PPARγ 具有抑制作用， IC50 分别为 6.3 nM 和 24 nM。BAY-0069 可用于研究癌症。
T35635	rac-trans-4-hydroxy Glyburide
	rac-trans-4-hydroxy Glyburide is an active metabolite of the SUR1/Kir6.2 sulfonylurea inhibitor glyburide .1,2It is formed from glyburide by the cytochrome P450 (CYP) isoforms CYP2C8 and CYP2C9.1rac-trans-4-hydroxy Glyburide inhibits glyburide binding to rat brain synaptosomes at the high and low affinity sites of SUR1/Kir6.2 with IC50values of 0.95 and 100 nM, respectively.2 1.Zharikova, O.L., Fokina, V.M., Nanovskaya, T.N., et al.Identification of the major human hepatic and placental enzymes ...
T35717	N-desmethyl Rosiglitazone
	N-desmethyl Rosiglitazone is a major metabolite of rosiglitazone , a potent and selective PPARγ ligand present in formulations that have been used to treat type 2 diabetes. Rosiglitazone is metabolized by the cytochrome P450 (CYP) isoform CYP2C8 to form N-desmethyl rosiglitazone.
T81744	mTOR inhibitor-14	mTOR	PI3K/Akt/mTOR signaling
	mTORinhibitor-14（compound 14c）是一种mTOR高效抑制剂，对CYP2C8的抑制作用较弱，并能有效抑制肿瘤生长。
T78590	Dibenzylfluorescein DBF
	Dibenzylfluorescein（DBF）是一款荧光探针，作为细胞色素P450（CYP）亚型，包括CYP3A4、CYP2C8、CYP2C9、CYP2C19和CYP19的特异性底物，常在Km值0.87-1.9 µM（Ex=485nm，Em=535nm）范围内应用。该探针主要用于监测药物或疾病导致的CYP催化活性变化。
T14040	4-Hydroxytolbutamide Hydroxytolbutamide	Potassium Channel	Membrane transporter/Ion channel
	4-Hydroxytolbutamide(Hydroxytolbutamide), a metabolite of Tolbutamide, which is metabolized by CYP2C8 and CYP2C9. Tolbutamide is a first generation potassium channel blocker and a sulfonylurea oral antidiabetic[1][2].
T36006	Olmesartan medoxomil impurity C
	Olmesartan medoxomil impurity C is an Olmesartan medoxomil impurity. Olmesartan medoxomil is a potent and selective angiotensin AT1 receptor inhibitor with IC50 of 66.2 μM. [1]. Senda A, et al. Effects of Angiotensin II Receptor Blockers on Metabolism of Arachidonic Acid via CYP2C8. Biol Pharm Bull. 2015;38(12):1975-9. [2]. Shah S, et al. Simultaneous Quantitative Analysis of Olmesartan Medoxomil and Amlodipine Besylate in Plasma by High-performance Liquid Chromatography Technique. J Young Phar...
T36085	PKI-179 hydrochloride
	PKI-179 is an orally bioavailable dual inhibitor of PI3K and mammalian target of rapamycin (mTOR). In an in vitro enzymatic assay, it potently inhibits PI3K (IC50s = 8, 24, 17, and 74 nM for isoforms α, β, δ, and γ, respectively), two common PI3Kα mutants, E545K and H1047R (IC50s = 14 and 11 nM, respectively), and mTOR (IC50 = 0.42 nM). PKI-179 is selective for PI3K and mTOR over a panel of 361 other kinases at IC50 values up to 50 μM, hERG (IC50 > 30 μM), and cytochrome P450 (CYP) isoforms (IC5...
T7788	2-Phenyl-2-(1-piperidinyl)propane	Others	Others
	2-Phenyl-2-(1-piperidinyl)propane 是一种具有可逆性、选择性的人 CYP2B6抑制剂，其 IC50为 5.1 μM，Ki 为 5.6。它对 CYP2D6 、CYP3A 均有抑制作用，且 IC50值分别为74 μM、200 μM。
T36084	PKI-179
	PKI-179 is a potent and orally active dual PI3K/mTOR inhibitor, with IC50s of 8 nM, 24 nM, 74 nM, 77 nM, and 0.42 nM for PI3K-α, PI3K-β, PI3K-γ, PI3K-δ and mTOR, respectively. PKI-179 also exhibits activity over E545K and H1047R, with IC50s of 14 nM and 11 nM, respectively. PKI-179 shows anti-tumor activity in vivo[1][2]. PKI-179 inhibits the cell proliferation, with IC50s of 22 nM and 29 nM for MDA361 and PC3 cells, respectively[1].PKI-179 shows inhibitory activity against a panel of 361 other ...

化合物

N-Desmethyl-Apalutamide

Cat.No: T12146

Synonym: N-Desmethyl Apalutamide,N-去甲基阿帕鲁胺杂质

Target: P450, Androgen Receptor

Carbamazepine 10,11-epoxide

Cat.No: T37149

Target: Others

Cat.No: T4567

Synonym: Plisulfan,Raziosulfa,Depocid,磺胺苯吡唑,Depotsulfonamide

Target: P450, Antibacterial

Cat.No: T41291

Target: P450

Cat.No: T1149

Synonym: Procetofen,非诺贝特,Lipanthyl,Lipantil

Target: P450, PPAR, Autophagy

3'-Hydroxy Repaglinide

Cat.No: T13497

Target: Others

Gemfibrozil 1-O-β-glucuronide

Cat.No: T11387

Target: Others

Cat.No: T67936

Target: PPAR

rac-trans-4-hydroxy Glyburide

Cat.No: T35635

N-desmethyl Rosiglitazone

Cat.No: T35717

mTOR inhibitor-14

Cat.No: T81744

Target: mTOR

Dibenzylfluorescein

Cat.No: T78590

Synonym: DBF

4-Hydroxytolbutamide

Cat.No: T14040

Synonym: Hydroxytolbutamide

Target: Potassium Channel

Olmesartan medoxomil impurity C

Cat.No: T36006

PKI-179 hydrochloride

Cat.No: T36085

2-Phenyl-2-(1-piperidinyl)propane

Cat.No: T7788

Target: Others

Cat.No: T36084

Cat. No.	Product Name	Target	Signaling Pathways
T10835	Cletoquine Desethylhydroxychloroquine	Parasite; Antifection	Microbiology/Virology
	Cletoquine 是 Hydroxychloroquine 的主要活性代谢物。 Cletoquine 具有对抗基孔肯雅病毒 (CHIKV) 的能力。 Cletoquine 具有抗疟作用，并具有治疗自身免疫性疾病的潜力。
T3149	Salvianolic Acid C 丹酚酸C,丹酚酸 C	Others; P450	Metabolism; Others
	Salvianolic acid C 是一种细胞色素 P4502C8(CYP2C8)的非竞争性抑制剂及细胞色素 P4502J2(CYP2J2)中等强度的混合抑制剂，对 CYP2C8 和 CYP2J2 的 Ki 分别为 4.82 μM 和 5.75 μM。

天然产物

Cat.No: T10835

Synonym: Desethylhydroxychloroquine

Target: Parasite, Antifection

Salvianolic Acid C

Cat.No: T3149

Synonym: 丹酚酸C,丹酚酸 C

Target: Others, P450

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