cytochrome b

Atovaquone (Atavaquone) 是具有口服活性的选择性寄生虫线粒体细胞色素bc1复合物的抑制剂。它抑制人类和P. falciparum 细胞色素bc1活性，IC50值分别为 460 nM 和 2.0 nM。它有抗疟作用，有潜力用于疟疾、弓形体病、肺孢子虫肺炎和巴贝斯虫病的相关研究。

Cytochrome P450 CYP1B1 (190-198) [Homo sapiens] is a peptide from Cytochrome c, which 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 positions1. Cytochrome c is a required cofactor for Apaf-1 function2.

Inz-1 是一种有效的真菌特异性线粒体细胞色素 bc1 抑制剂，对酵母和人类的 IC50 分别为 8.092 和 45.320 μM。 Inz-1 可逆转氟康唑或其他三唑类抗真菌药对致病性真菌白色念珠菌的耐药性。

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。

Quinidine sulfate dihydrate (Pitayine Sodium) 是抗心律失常剂，能够阻断 K+通道(IC50:19.9 μM)。它是细胞色素 P450db 的选择性抑制剂，可用于研究疟疾。

Pyribencarb，一种苯甲酰胺类杀菌剂，针对多种植物病原真菌展现出广谱活性。作为细胞色素b的强效Qo抑制剂，Pyribencarb 对灰霉病菌（Botrytis cinerea）和菌核病菌（Sclerotinia sclerotiorum）特别有效。

Nampt-IN-5 是烟酰胺磷酸核糖基转移酶抑制剂。它可抑制 A2780 和 COR-L23 细胞，IC50值分别为 0.7 nM 和 3.9 nM。它还抑制 CYP3A4 活性。

Pradefovir mesylate (Hepavir B) 是一种肝脏 CYP3A4 底物。在人肝微粒体中，Pradefovir 能够转化为 9-[2-(磷酸甲氧基)乙基]腺嘌呤，其Km=60 μM。

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)

Clindamycin sulfoxide is an active metabolite of the antibiotic clindamycin . It is formed via S-oxidation of clindamycin primarily by the cytochrome P450 (CYP) isoform CYP3A4. Clindamycin sulfoxide inhibits the growth of P. prevotti, B. fragilis, and C. sordelli in vitro with MIC values of 2, 2, and 1 mg L, respectively.

N-hydroxy Riluzole is a metabolite of the antiglutamatergic agent riluzole .1It is formed from riluzole predominantly by the cytochrome P450 (CYP) isoform CYP1A2 in human hepatic microsomes. 1.Sanderink, G.J., Bournique, B., Stevens, J., et al.Involvement of human CYP1A isoenzymes in the metabolism and drug interactions of riluzole in vitroJ. Pharmacol. Exp. Ther.282(3)1465-1472(1997)

17R(18S)-EpETE is an oxylipin and a cytochrome P450 metabolite of eicosapentaenoic acid .1,217R(18S)-EpETE is an activator of large-conductance calcium-activated potassium (BKCa) channels, increasing the potassium current amplitude by 15-fold in isolated rat cerebral artery vascular smooth muscle cells (VSMCs) at +60 mV when used at a concentration of 50 nM.2It has negative chronotropic effects in isolated neonatal rat cardiomyocytes (NRCMs; EC50= ~1-2 nM) and prevents calcium-induced increases in the spontaneous beating of NRCMs.3,4 1.Schwarz, D., Kisselev, P., Ericksen, S.S., et al.Arachidonic and eicosapentaenoic acid metabolism by human CYP1A1: Highly steroselective formation of 17(R), 18(S)-epoxyeicosatetraenoic acidBiochem. Pharmacol.67(8)1445-1457(2004) 2.Lauterbach, B., Barbosa-Sicard, E., Wang, M.H., et al.Cytochrome P450-dependent eicosapentaenoic acid metabolites are novel BK channel activatorsHypertension39(2 Pt. 2)609-613(2002) 3.Falck, J.R., Wallukat, G., Puli, N., et al.17(R),18(S)-Epoxyeicosatetraenoic acid, a potent eicosapentaenoic acid (EPA) derived regulator of cardiomyocyte contraction: Structure-activity relationships and stable analoguesJ. Med. Chem.54(12)4109-4118(2011) 4.Arnold, C., Markovic, M., Blossey, K., et al.Arachidonic acid-metabolizing cytochrome P450 enzymes are targets of omega-3 fatty acidsJ. Biol. Chem.285(43)32720-32733(2010)

Dehydro Nifedipine (BAY-b 4759) 是人血浆中硝苯地平的主要代谢物。Dehydro Nifedipine 抑制PC-12细胞葡萄糖摄取，IC50值为130 μM，硝苯地平是一种钙通道阻滞剂，用于治疗高血压和心绞痛。当硝苯地平被细胞色素P450 (CYP)异构体CYP3A4和CYP3A5代谢时形成脱氢硝苯地平。

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 inhibitor of the cytochrome P450 (CYP) isoform CYP3A4 (Ki = 15 μM in human liver microsomes).

Methyl protodioscin (Smilax saponin B) 是一种甾二糖苷，能诱导细胞周期阻滞，具有抗肿瘤活性。

Picoxystrobin, a prominent primary strobilurin fungicide, is extensively utilized for efficient plant disease management. By obstructing electron transfer at the Qo center of cytochrome b and c1, picoxystrobin effectively halts mitochondrial respiration[1].

Q203 (Telacebec)是一种中氮杂吡啶酰胺。 在培养基中抑制结核分枝杆菌H37Rv 活性的MIC50值为2.7 nM。

β-​Apo-​8'-​carotenal (Apocarotenal) 是一种存在于许多蔬菜、水果中的维生素原 A 类胡萝卜素，是大鼠CYP1A1和CYP1A2的诱导剂。

Schisandrol B (Besigomsin) 是华中五味子的主要活性成分，具有保肝、抗炎、抗糖尿病和抗氧化的作用。它抑制活性氧的产生，也抑制 P-糖蛋白和CYP3A 的活性。

Azalanstat HCl is an anti-obesity drug acting as a lanosterol 14α-demethylase inhibitor. Azalanstat HCl 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 density lipoprotein (LDL) cholesterol and apo B relative to high density lipoprotein (HDL) cholesterol and apo A-1.

Azalanstat mesylate is an anti-obesity drug acting as a lanosterol 14α-demethylase inhibitor. Azalanstat mesylate 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 density lipoprotein (LDL) cholesterol and apo B relative to high density lipoprotein (HDL) cholesterol and apo A-1.

11α-Hydroxy Testosterone, a testosterone metabolite, is synthesized by the cytochrome P450 (CYP) isoform CYP3A.1, and can alternatively be produced from testosterone by a CYP107A1 mutant or from 11α-hydroxy progesterone by the fungus B. bassiana.2,3 The biological activity of 11α-Hydroxy Testosterone remains unclear.

N-Desmethyl Regorafenib N-oxide, an active metabolite of the multi-kinase inhibitor regorafenib, originates through the action of the cytochrome P450 (CYP) isoform CYP3A4. This compound demonstrates efficacy in vitro by inhibiting key enzymes such as VEGFR2, Tie2, c-Kit, and B-RAF, and it exhibits tumor growth inhibition in HT-29 and MDA-MB-231 mouse xenograft models at a dosage of 1 mg/kg.

Cyprocide-B在经Cytochrome P450激活后会转变为亲电性代谢物,能特异性地消灭线虫C. elegans.该化合物为开发选择性杀线虫剂提供了研究基础.