liver cytochrome

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。

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。

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。

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。

Protoporphyrin IX (PPIX) 是一种四吡咯，是血红素、细胞色素 c 和叶绿素的代谢前体。Protoporphyrin IX 具有改善肝脏机能、促进细胞组织呼吸、改善蛋白质和糖代谢、抗补体结合等作用。

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。

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。

Phoxim（辛硫磷）是一种有机磷酸酯类杀虫剂，抑制昆虫神经系统中的乙酰胆碱酯酶（AchE）活性。在兽医学中用于治疗外寄生螨虫。对水生生物具有毒性，可能影响鱼类肝脏微粒体中细胞色素P450酶（CYP1A）的活性及其表达水平。​此外，亚致死剂量的辛硫磷也会影响桑粉虱成虫的解毒酶活性，如谷胱甘肽S-转移酶（GST）、羧酸酯酶（CarE）和乙酰胆碱酯酶（AchE）的活性变化。

Hydroxy desmethyl Bosentan (Ro 64-105) is a Bosentan metabolism produced by the cytochrome P450 enzymes CYP2C9 and CYP3A4 in the liver.

O-Desmethyl Midostaurin is the active Midostaurin metabolite via cytochrome P450 liver enzyme metabolism.

(-)-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。

(+)-Cevimeline hydrochloride hemihydrate ((+)-SNI-2011) 是一种有效的 mAChR 激动剂。

Hydroxy bosentan (Ro 48-5033) is a primary metabolite of Bosentan (BOS) metabolized by the cytochrome P450 system in the liver, assisting BOS pharmacologically with 10%-20% activity retention.

Antifungal agent 114 (Compound 19g) 作为一种强效的细胞色素 P450 (Cytochrome P450) 抑制剂，在10 μM 浓度下能够有效抑制 CYP2C9、CYP2C19、CYP2D6 和 CYP3A4。此外，该化合物对 Cryptococcus neoformans、Candida 和 Aspergillus 显示出显著的抗真菌活性，其最小抑菌浓度（MIC）低于0.0625 μg mL。在人类肝微粒体中，Antifungal agent 114 展现出优良的代谢稳定性，其半衰期达到107分钟。

SM 12502 是人类肝微粒体中细胞色素P450 2A6的底物。

TG-100435是一种新型的多靶点口服蛋白酪氨酸激酶抑制剂。TG100435的代谢通量会被甲巯咪唑和酮康唑完全抑制。在人类肝微粒体或重组P450中，TG100435的形成随细胞色素P450还原酶活性的增加而增加，暗示着细胞色素P450还原酶可能参与其中。

Octachlorodibenzo-p-dioxin (OCDD) 是一种环境污染物，但没有急性给药毒性。在大鼠体内，Octachlorodibenzo-p-dioxin 通过静脉注射 (50 μg kg i.v.) 或口服 (50-5000 μg kg p.o.) 的全身消除半衰期为 3-5 个月，在低剂量的多次暴露后会在肝脏和脂肪组织中累积和浓缩。重复给药后，Octachlorodibenzo-p-dioxin 会导致7-乙氧基异噻唑啉-O-脱乙基酶 (7-ethoxyresorufin-O-deethylase, 7-EROD) 活性增加，以及总细胞色素P-450水平升高。

Erythromycin glutamate is a macrolide bacteriostatic antibiotic. This antibiotic is metabolized through the liver and inhibits cytochrome enzyme P450A 3A41.

(±)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 of the area at risk in a canine model of ischemia-reperfusion injury induced by left anterior descending coronary artery (LAD) occlusion when administered at a dose of 0.128 mg kg prior to occlusion or reperfusion.[5] Reference：[1]. Chacos, N., Falck, J.R., Wixtrom, C., et al. Novel epoxides formed during the liver cytochrome P-450 oxidation of arachidonic acid. Biochem. Biophys. Res. Commun. 104(3), 916-922 (1982).[2]. Oliw, E.H., Guengerich, F.P., and Oates, J.A. Oxygenation of arachidonic acid by hepatic monooxygenases. Isolation and metabolism of four epoxide intermediates. J. Biol. Chem. 257(7), 3771-3781 (1982).[3]. Jiang, J.-X., Zhang, S.-J., Xiong, Y.-K., et al. EETs attenuate ox-LDL-induced LTB4 production and activity by inhibiting p38 MAPK phosphorylation and 5-LO BLT1 receptor expression in rat pulmonary arterial endothelial cells. PLoS One 10(6), e0128278 (2015).[4]. Oltman, C.L., Weintraub, N.L., VanRollins, M., et al. Epoxyeicosatrienoic acids and dihydroxyeicosatrienoic acids are potent vasodilators in the canine coronary microcirculation. Circ. Res. 83(9), 932-939 (1998).[5]. Nithipatikom, K., Moore, J.M., Isbell, M.A., et al. Epoxyeicosatrienoic acids in cardioprotection: Ischemic versus reperfusion injury. Am. J. Physiol. Heart Circ. Physiol. 291(2), H537-H542 (2006).

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, NADH oxidase, α-glycerophosphate dehydrogenase, isocitrate dehydrogenase, and malate dehydrogenase in rats.3 1.Moubasher, A.H., el-Kady, I.A., and Shoriet, A.Toxigenic Aspergilli isolated from different sources in EgyptAnn. Nutr. Aliment.31(4-6)607-615(1977) 2.Wogan, G.N., Edwards, G.S., and Newberne, P.M.Structure-activity relationships in toxicity and carcinogenicity of aflatoxins and analogsCancer Res.31(12)1936-1942(1971) 3.Bai, N.J., Pai, M.R., and Venkitasubramanian, T.A.Mitochondrial function in aflatoxin toxicityIndian J. Biochem. Biophys.14(4)347-349(1977)

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)

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)

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.

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 a substrate for Glutathione S-transferase, microsomal epoxide hydrolase and porcine liver carboxylesterase. Hydrolysis of S-NEPC by sEH yields 4-nitrophenol which can be quantified spectrophotometrically at 405 nm. S-NEPC is adaptable for use in 96-well microwell plate readers.