cyp 19

CYP19A1 CYP11B2-IN-1 (Compound X21) 是一种高效且选择性的芳香化酶和醛固酮合酶双重抑制剂，具备针对aromatase (CYP19A1)和aldosterone synthase (CYP11B2)的低IC50值，分别为2.3 nM和29 nM。此化合物在抑制癌细胞增殖和促进细胞凋亡方面表现出色，适合用于乳腺癌的科学研究。

YM 511 是一种高度特异性的非甾体芳香酶 (aromatase) 抑制剂。YM 511 竞争性抑制大鼠卵巢和人胎盘微粒体中的芳香酶活性 (IC50 分别为 0.4 和 0.12 nM)。YM 511 轻微抑制其他类固醇激素的产生。YM 511 具有用于抑制雌激素依赖性作用研究，不会影响其他类固醇激素的血清水平的潜力。

CYP2C9 CYP2C19-IN-1 是无肝脏毒性和遗传毒性的CYP2C9 CYP2C19强效抑制剂，能够用于研究寨卡病毒 (ZIKV) 感染。

CYP2C19-IN-1 是强效的，无遗传毒性的、无肝脏毒性的 CYP2C19 抑制剂。 CYP2C19-IN-1 能够抑制 RNA 依赖的 RNA 聚合酶 (RdRP) (Ki: 6.16 μM)，能够用于研究寨卡病毒 (ZIKV) 感染。

CYP51-IN-19(compound C07)为一种高效CYP51抑制剂,能够激发活性氧(ROS),展示出显著的抗真菌活性.

CYP2C1 CYP2C19-IN-2 是无肝脏毒性和遗传毒性的CYP2C9 CYP2C19强效抑制剂，能够用于研究寨卡病毒 (ZIKV) 感染。

7-Hydroxyflavanone 对肺炎链球菌临床分离株显示出抗菌活性。

2-Naphthol-d8 是 2-Naphthol 的氘代化合物。2-Naphthol 的 CAS 号为 135-19-3。2-Naphthol 是一种 naphthalene 的代谢物，由细胞色素 P450 亚型 (CYP 1A1，CYP 1A2，CYP 2A1，CYP 2E1 和 CYP 2F2) 催化而成。2-Naphthol 具有细胞毒性。

CYP4A11 CYP4F2-IN-1 是一种高效的小分子细胞色素 P450 (CYP) 4A11 和 CYP4F2 抑制剂，对P450 (CYP) 4A11 的 IC50 值为 19 nM，对 CYP4F2 的 IC50 值为 17 nM。CYP4A11 CYP4F2-IN-1 可用于研究肾脏疾病和心脑血管疾病。

(±)19(20)-EpDTE is an oxylipin and an oxidative metabolite of docosapentaenoic acid . It is formed via cytochrome P450 (CYP) metabolism of DPA and can be further metabolized to (±)19(20)-DiHDTE by epoxide hydrolase.

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.

CAY10770 is an inhibitor of the cytochrome P450 (CYP) isoform CYP4Z1 (IC50= 5.9 μM).1It is selective for CYP4Z1 over CYP4A11, CYP4F2, CYP4F3a, CYP4F3b (IC50s = 187-282 μM) but does inhibit CYP4F8 and CYP4F12 (IC50s = 167 and 91 μM, respectively). CAY10770 (3 μM) inhibits the production of 14(15)-EET, 19-HETE, and 14(15)-DiHET by 83, 86, and 80%, respectively, in T47D breast cancer cells expressing CYP4Z1. 1.Kowalski, J.P., McDonald, M.G., Pelletier, R.D., et al.Design and characterization of the first selective and potent mechanism-based inhibitor of cytochrome P450 4Z1J. Med. Chem.63(9)4824-4836(2020)

(±)19(20)-EDP ethanolamide is an ω-3 endocannabinoid epoxide and cannabinoid (CB) receptor agonist (EC50s = 108 and 280 nM for CB1 and CB2, respectively). It is produced through direct epoxygenation of docosahexaenoyl ethanolamide by cytochrome P450 (CYP) epoxygenases. (±)19(20)-EDP ethanolamide (25 μM) reduces the viability of 143B metastatic osteosarcoma cells. It decreases the production of IL-6 and increases the production of IL-10 when used at concentrations ranging from 2.5 to 10 μM in BV-2 microglia stimulated by LPS and decreases LPS-induced cytotoxicity when used at concentrations ranging from 5 to 10 μM. It also decreases nitrite production when used at a concentration of 7.5 μM, an effect that can be partially reversed by the CB2 receptor antagonist AM630 and the PPARγ antagonist GW 9662 . (±)19(20)-EDP ethanolamide induces vasodilation of isolated preconstricted bovine coronary arteries (ED50 = 1.9 μM) and reduces tube formation by human microvascular endothelial cells (HMVECs) in a Matrigel assay.

(±)19(20)-DiHDTE is an oxylipin and an oxidative metabolite of docosapentaenoic acid . It is formed via cytochrome P450 (CYP) metabolism of DPA via a (±)19(20)-EpDTE intermediate.