奥美沙坦

中文名称:

奥美沙坦

中文同义词:

奥美沙坦;4-(1-羟基-1-甲基乙基)-2-丙基-1-[2-(四唑-5-基)苯基]苯基]甲基咪唑-5-羧酸;奥美沙坦酯杂质A (EP);奥美沙坦酸(奥美沙坦EP杂质A);奥美沙坦溶液,100PPM;奥美沙坦溶液,1000PPM;美沙坦酯杂质A;奥美沙坦酯A

英文名称:

Olmesartan

英文同义词:

4-(1-Hydroxy-1-methylethyl)-2-propyl-1-[[2-(1H-tetrazol-5-yl)[1,1-biphenyl]-4-yl]methyl]-1H-imidazole-5-carboxylic acid;Olmesartan;4-(1-Hydroxy-1-methylethyl)-2-propyl-1-[[2’-(1H-tetazol-5-yl)[1,1’-biphenyl]-4-yl]methyl]-1H-imidazole-5-carboxylic Acid;CS 088;Olmesartan Acid;Olmesartan Medoxomil-1;CS-415;Olmesartan (Olmesartan Medoxomil EP Impurity A)

CAS号:

144689-24-7

分子式:

C24H26N6O3

分子量:

446.5

EINECS号:

646-413-5

相关类别:

中药对照品;标准品;G蛋白偶联受体G蛋白;医药原料;抗生素类;原料药中间体;食品添加剂;Bases Related Reagents;Intermediates Fine Chemicals;Nucleotides;Pharmaceuticals;Isotope Labeled Compounds;高血压用药;对照品-杂质对照品;化工原料;杂质对照品

Mol文件:

144689-24-7.mol

熔点 

186-188°C

沸点 

738.3±70.0 °C(Predicted)

密度 

1.33

储存条件 

2-8°C

酸度系数(pKa)

2.39±0.50(Predicted)

形态

powder

颜色

white to beige

CAS 数据库

144689-24-7(CAS DataBase Reference)

概述

奥美沙坦是奥美沙坦酯EP杂质A。奥美沙坦酯是新的血管紧张素∏(AT∏)受体拮抗剂，2002年5月首次获得美国 FDA 批准上市用于治疗高血压。

生物活性

Olmesartan (RNH-6270) 是血管紧张素II受体 (AT1R) 拮抗剂，常用于高血压的相关研究。

体外研究

Olmesartan (0.7-5 mM; 24, 48 and 72 h) inhibits the growth of HeLa cells as a concentration- and time-dependent mode. Cell Viability Assay Cell Line: Human cervical cancer cell line (HeLa) Concentration: 0.7- 5 mM Incubation Time: 24, 48 and 72 h Result: IC 50 s against HeLa cell line are 4.685 and 1.651 mM for 48 and 72 h, respectively.

Cell Line:

Human cervical cancer cell line (HeLa)

Concentration:

0.7- 5 mM

Incubation Time:

24, 48 and 72 h

Result:

IC 50 s against HeLa cell line are 4.685 and 1.651 mM for 48 and 72 h, respectively.

体内研究

Repeated dosing of olmesartan (1 mg/kg, 2 mg/kg, p.o.) dose-dependently decreases mean arterial blood pressure (MAP) in SHR without significant influence on body weight and food intake during 10 weeks. Olmesartan (5 mg/kg/d, p.o.) and Hyd treatments lower systolic blood pressure to the same degree in mice. Olmesartan treatment inhibits cardiac hypertrophy, evaluated by echocardiography, heart weight, cross-sectional area of cardiomyocytes, and gene expression. Olmesartan treatment reverses decreased gene expressions of ACE2 and Mas receptor of Ren-Tg mice and inhibits enhanced NADPH oxidase (Nox)4 expression and reactive oxygen species.

用途 

高血压,在治疗高血压病的各类药物中,ARB之所以成为应用比例上升最快的药物,其重要原因是该类药物的有效性和良好的安全性(妊娠妇女除外)

RTECS号

NI4014100

海关编码 

29339900