cyp2c8

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。

Gemfibrozil 1-O-β-Glucuronide, a metabolite of Gemfibrozil, is a potent and competitive inhibitor of P450 (CYP) isoform CYP2C8, with an IC50 of 4.07 μM.

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。

Fenofibrate (Lipanthyl) 是一种 PPARα 激动剂 (EC50=30 μM)，具有选择性。Fenofibrate 还抑制细胞色素 P450 亚型，如 CYP2C19、CYP2B6、CYP2C9、CYP2C8 和 CYP3A4。Fenofibrate 具有抗高血脂活性。

Mertansine 是一种微管蛋白抑制剂，也是一种抗体可缀合的美登木素生物碱。Mertansine 对HCT-15和A431细胞的IC50分别是0.750和0.04nM。

Apinocaltamide(ACT-709478)是一种可口服和选择性的T型Ca 2+ 通道 (T-type calcium channel) 阻滞剂，具有可透过血脑屏障（BBB）的特性，对Cav3.1, Cav3.2和 Cav3.3的IC50=6.4~18nM，常用于癫痫的研究。

BMS-986339 是一种具有口服活性的FXR 激动剂。BMS-986339 可与 His298 和 ASN287 残基形成氢键。BMS-986339 可用于原发性胆汁性肝硬化 (PBC)、原发性硬化性胆管炎 (PSC)、非酒精性脂肪性肝炎 (NASH)，和抗纤维化研究。

DL-Acetylshikonin can effectively inhibit tumor cells, it can be used to treat hepatocellular carcinoma cells expressing hepatitis B virus X protein (HBX) by inducing ER stress , an oncoprotein from hepatitis B virus. Acetylshikonin inhibits the production of eicosanoid, is due to the attenuation of cytosolic phospholipase A(2) membrane recruitment via the decrease in [Ca(2+)](i) and to the blockade of cyclooxygenase and 5-lipoxygenase activity.

Thujopsene, a sesquiterpene found in T. dolabrata, exhibits a wide range of biological activities. It inhibits Na+ K+-ATPase and cytochrome P450 (CYP) isoform CYP2B6 with IC50 values of 25.9 µg ml and Ki of 0.8 µM, respectively. Additionally, thujopsene demonstrates antimicrobial efficacy against both Gram-positive and Gram-negative bacteria, such as S. aureus, M. luteus, and S. typhimurium, with MICs ranging from 25-50 µg ml. It also suppresses antigen-induced β-hexosaminidase release in IgE-sensitized RBL-2H3 mast cells (IC50= 25.1 µM) and shows cytotoxicity against A549 non-small cell lung cancer cells with an LC50 of 35.27 µg ml. Furthermore, thujopsene causes mortality in mites D. farinae and T. putrescentiae, with LC50s of 9.82 and 10.92 µg cm2, respectively.

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。

Salvianolic acid C 属于天然产物，是一种细胞色素 P4502C8(CYP2C8) 和细胞色素 P4502J2(CYP2J2) 的抑制剂 (Ki=4.82 5.75 μM)，具有非竞争性。Salvianolic Acid C 具有抗新冠病毒活性。

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。

'3'-Hydroxy Repaglinide, a primary CYP2C8 metabolite of Repaglinide, is derived from carbamoylmethyl benzoic acid and is used in the treatment of type II diabetes.

4-Hydroxytolbutamide(4-羟基甲苯磺丁脲)是一种磺脲和药物代谢物，由 CYP2C8 和 CYP2C9 代谢Tolbutamide得到。Tolbutamide (HLS 831) 是一种磺脲类降糖药。

Lesinurad sodium (RDEA594 sodium) 是一种具有选择性的尿酸重吸收抑制剂，可用于研究心血管疾病。

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 responsible for the biotransformation of glyburideBiochem. Pharmacol.78(12)1483-1490(2009) 2.Hill, R.A., Rudra, S., Peng, B., et al.Hydroxyl-substituted sulfonylureas as potent inhibitors of specific [3H]glyburide binding to rat brain synaptosomesBioorg. Med. Chem.11(9)2099-2113(2003)

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.

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 Pharm. 2012 Apr;4(2):88-94.

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 kinases, hERG and cytochrome P450 (CYP) isoforms at concentrations up to >30 μM, but does have activity for CYP2C8 (IC50=3 μM)[1]. PKI-179 (5-50 mg kg; p.o. once daily for 40 days) inhibits the tumor growth and is well tolerated in nude mice bearing MDA-361 human breast cancer tumors[1].PKI-179 (50 mg kg; p.o.) results in good inhibition of PI3K signaling in nude mice bearing MDA361 tumor xenografts[1].PKI-179 exhibits good oral bioavailability (98% in nude mouse, 46% in rat, 38% in monkey, and 61% in dog) and a high half-life (>60 min) [1]. [1]. Venkatesan AM, et, al. PKI-179: an orally efficacious dual phosphatidylinositol-3-kinase (PI3K) mammalian target of rapamycin (mTOR) inhibitor. Bioorg Med Chem Lett. 2010 Oct 1;20(19):5869-73.[2]. Rehan M. A structural insight into the inhibitory mechanism of an orally active PI3K mTOR dual inhibitor, PKI-179 using computational approaches. J Mol Graph Model. 2015 Nov;62:226-234.

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 (IC50s > 30 μM), but does have activity for CYP2C8 (IC50 = 3 μM). It inhibits proliferation through the Akt/mTOR signaling pathway in MDA-361 breast and PC3MM2 prostate cancer cell lines in vitro (IC50s = 22 and 29 nM, respectively) and inhibits tumor growth in an MDA-361 mouse xenograft model when used at a dose of 50 mg/kg.

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。

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。

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。

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。