常用名 | 罗伐他汀 | CAS号 | 287714-41-4 |
---|---|---|---|
价格 | ¥8586.0/25g ¥386.0/250mg ¥776.0/1g ¥5146.0/10g | 纯度 | 95.0% |
备货期 | 1天 | 库存 | 询单 |
产品详情(用途,包装等)
用途: Rosuvastatin is a competitive inhibitor of HMG-CoA reductase with IC50 of 11 nM. IC50 Value: 11 nM [1]Target: HMG-CoA reductasein vitro: Rosuvastatin is relatively hydrophilic and is highly selective for hepatic cells; its uptake is mediated by the liver-specific organic anion transporter OATP-C. Rosuvastatin is a high-affinity substrate for OATP-C with apparent association constant of 8.5 μM [2]. Rosuvastatin inhibits cholesterol biosynthesis in rat liver isolated hepatocytes with IC50 of 1.12 nM. Rosuvastatin causes approximately 10 times greater increase of mRNA of LDL receptors than pravastatin [1]. Rosuvastatin (100 μM) decreases the extent of U937 adhesion to TNF-α-stimulated HUVEC. Rosuvastatin inhibits the expressions of ICAM-1, MCP-1, IL-8, IL-6, and COX-2 mRNA and protein levels through inhibition of c-Jun N-terminal kinase and nuclear factor-kB in endothelial cells [3].in vivo: Rosuvastatin (3 mg/kg) daily administration for 14 days decreases plasma cholesterol levels by 26% in male beagle dogs with normal cholesterol levels. In cynomolgus monkeys, Rosuvastatin decreases plasma cholesterol levels by 22% [1]. Rosuvastatin (20 mg/kg/day) administration for 2 weeks, significantly reduces very low-density lipoproteins (VLDL) in diabetes mellitus rats induced by Streptozocin [4]. Rosuvastatin shows antiatherothromhotic effects in vivo. Rosuvastatin (1.25 mg/kg) significantly inhibits thrombin-induced transmigration of monocvtes across mesenteric venules via inhibition of the endothelial cell surface expression of P-selectin, and increases the basal rate of nitric oxide in aortic segments by 2-fold times [5]. 物理化学性质: CAS号:287714-41-4 常用中文名:罗伐他汀 常用英文名:Rosuvastatin 分子式:C22H28FN3O6S 分子量:481.54 密度:1.368 g/cm3 沸点:745.6ºC at 760 mmHg 熔点:N/A 闪点:404.7ºC 储存条件:2-8°C |