cyp4a11

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。

CYP4A11 CYP4F2-IN-2（compound 15）作为一种口服抑制剂，其针对CYP4A11及CYP4F2 的IC50s 分别为 120 nM 和 220 nM。该化合物能够有效抑制大鼠肾中的20-HETE生成，显示出对尿病肾病和常染色体显性多囊肾病治疗的潜力。

TP0472993 是一种有效的和具有口服活性的细胞色素 P450 (CYP) 4A11 和 CYP4F2 的双重抑制剂，IC50 值分别为 140 nM 和 40 nM。TP0472993 可从肝脏和肾脏中提取， 具有治疗肾脏疾病的潜力。

17β-hydroxy Exemestane is the primary active metabolite of exemestane . It is formed by metabolism of exemestane by the cytochrome P450 (CYP) isoforms CYP1A and CYP4A11. 17β-hydroxy Exemestane is an aromatase inhibitor (IC50 = 69 nM using human placental microsomes) and an androgen receptor (AR) agonist (IC50 = 39.6 nM) that is selective for AR over estrogen receptor α (ERα; IC50 = 21.2 μM). It stimulates growth of AR- and ERα-positive MCF-7 (EC50 = 2.7 μM) and T47D breast cancer cells (EC50s = 0.43 and 1,500 nM for AR- and ER-mediated growth, respectively) and inhibits proliferation of testosterone-treated aromatase-overexpressing MCF-7aro cells in a concentration-dependent manner. 17β-hydroxy Exemestane (20 mg/kg) inhibits increases in serum cholesterol and LDL levels and prevents decreases in bone mineral density in the lumbar vertebrae and femur, as well as femoral bending strength and compressive strength of the fifth lumbar vertebrae, in ovariectomized rats.

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)

CAY10462 (CTK8E8405) 是一种有效的 20-HETE 合酶 CYP4A11 的选择性抑制剂，IC50 为 8.8 nM。 CAY10462 对 1A、1C 和 3A CYP450 酶的效力降低近 200 倍。