20-hete

20-HETE 促进癌症中的细胞增殖和迁移，通过激活蛋白激酶 C 通路以增加 FBXO10 的表达，可用于研究前列腺肿瘤和心脏肥大。

Alkynyl Stearic Acid 是 CYP450 ω-羟化酶抑制剂。它能够抑制与花生四烯酸孵育的大鼠肾皮质微粒体形成 20-HETE 、dihydroxyeicosatrienoic acids、epoxyeicosatrienoic acids。它可以改善异丙肾上腺素诱导的培养心肌细胞凋亡和坏死。

20-HETE Intermediate 15 是20-羟基二十碳四烯酸的中间体。

20-HETE inhibitor-1（comp 83）为一种20-HETE合成过程中的抑制剂。

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。

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。

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。

HET0016 is a potent and selective 20-HETE synthase inhibitor [IC50s: 17.7 nM, 12.1 nM, and 20.6 nM for recombinant CYP4A1-, CYP4A2- and CYP4A3-catalyzed 20-HETE synthesis]. HET0016 is also a selective CYP450 inhibitor shown to inhibit angi.

N-(3-Chloro-4-morpholinophenyl)-N'-hydroxyformimidamide (TS-011) 是一种选择性 20-羟基二十碳四烯酸合成抑制剂。

20-HEDE (WIT 002) is a 20-hydroxyeicosatetraenoic acid (20-HETE) antagonist.

AAA is an antagonist of G protein-coupled receptor 75 (GPR75).1It increases basal GPR75 protein levels and inhibits 20-HETE-induced reductions in GPR75 protein levels in PC3 cells. AAA (5 and 10 μM) also reduces 20-HETE-induced phosphorylation of EGFR, NF-κB, and Akt in, and cell migration of, PC3 cells.In vivo, AAA (10 mg/kg per day) reduces systolic blood pressure, albuminuria, renal angiotensin II levels, and cardiac hypertrophy in a Cyp1a1-Ren-2 transgenic rat model of malignant hypertension when administered prior to induction or after establishment of hypertension.2 1.Cárdenas, S., Colombero, C., Panelo, L., et al.GPR75 receptor mediates 20-HETE-signaling and metastatic features of androgen-insensitive prostate cancer cellsBiochim. Biophys. Acta Mol. Cell Biol. Lipids1865(2)158573(2020) 2.Sedláková, L., Kikerlová, S., Husková, Z., et al.20-Hydroxyeicosatetraenoic acid antagonist attenuates the development of malignant hypertension and reverses it once established: a study in Cyp1a1-Ren-2 transgenic ratsBiosci. Rep.38(5)BSR20171496(2018)

20-carboxy Arachidonic acid (20-COOH-AA) is the major metabolite of 20-HETE that is produced in renal tubular epithelial, endothelial, and microvascular smooth muscle cell cultures. This ω-oxidation conversion can take place using purified alcohol dehydrogenases three and four or by microsomes containing recombinant human CYP4F3B. Like 20-HETE, 20-COOH-AA inhibits ion transport in the kidneys. It also produces vasorelaxation of porcine coronary microvessels constricted with endothelin. 20-COOH-AA binds to isolated ligand binding domains of peroxisome proliferator-activated receptor α (PPARα) (Kd = 0.87 ± 0.12 μM) and PPARγ (Kd = 1.7 ± 0.5 μM), and is a dual activator of PPARα and PPARγ in a transiently transfected COS-7 cell reporter system.

20-5,14-HEDGE 是 20-HETE 类似物，对大鼠肺缺血再灌注损伤有保护作用。

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。