| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| R408257-1ml |
1ml |
现货  |
|
| 英文别名 | calcium (3R,5S,E)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethan-3-ylsulfonamido)pyrimidin-5-yl)-3,5-dihydroxyhept-6-enoate |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Rosuvastatin (ZD4522) calcium |
| 生化机理 | 瑞舒伐他汀钙片（ZD4522）是一种 HMG-CoA 还原酶竞争性抑制剂，在无细胞试验中的 IC50 值为 11 nM。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | HMG-CoA 还原酶抑制剂 |
| 产品介绍 |
Rosuvastatin Calcium是一种竞争性HMG-CoA还原酶抑制剂， with IC50为11 nM。A selective and competitive inhibitor of HMG-CoA reductase. Information Rosuvastatin Calcium (ZD4522) is a competitive inhibitor ofHMG-CoA reductasewithIC50of 11 nM in a cell-free assay. 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. 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. 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. In vivo Rosuvastatin is efficient on reducing plasma liquids. 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% Rosuvastatin (20 mg/kg/day) administration for 2 weeks, significantly reduces very low-density lipoproteins (VLDL) in diabetes mellitus rats induced by Streptozocin. 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. Rosuvastatin (20 mg/kg) inhibits ROS production, normalizes NO-dependent endothelial function and reduces platelet activation in diabetic rats induced by Streptozocin. Rosuvastatin displays cardioprotective effects in vivo. Rosuvastatin (80 mg) is shows to decrease infarct size and improve cardiac mechanical function after ischemia/reperfusion in animal model. The cardioprotective properties of Rosuvastatin may be due to the improvement of coronary blood flow, decrease in resistance of coronary arteries mediated by enhanced eNOS expression, and the subsequent increase in the production of vascular endothelial NO. Rosuvastatin (2.0 mg/kg) attenuates left ventricular hypertrophy produced by transaortic constriction in mice through regulation of Racl protein and NADPH oxidase activities. cell lines：HL-60, U937, and NB-4 cells Concentrations： Incubation Time： Powder Purity:≥99% |
| Isomeric SMILES | CC(C1=NC(=NC(=C1/C=C/[C@@H](O)C[C@@H](O)CC(=O)[O-])C2=CC=C(C=C2)F)N(S(=O)(=O)C)C)C.CC(C1=NC(=NC(=C1/C=C/[C@@H](O)C[C@@H](O)CC(=O)[O-])C2=CC=C(C=C2)F)N(S(=O)(=O)C)C)C.[Ca+2] |
|---|---|
| PubChem CID | 5282455 |
| 分子量 | 500.57 |
| 溶解性 | Solubility (25°C) In vitro Water: 5 mg/mL (38.11 mM); DMSO: Insoluble; |
|---|---|
| 比旋光度 | -8° (C=1,CHCl3) |
| 熔点 | 160 °C |
| 象形图 | GHS08, GHS09 |
|---|---|
| 信号词 | Danger |
| 危险声明 |
H410: 对水生生物有剧毒并具有长期持续影响 H372: 通过长时间或反复暴露对器官造成损害 H360: 可能损害生育力或未出生的孩子 H350: 可能导致癌症 H370: 对器官造成损害 H362: 可能对母乳喂养的孩子造成伤害 |
| 预防措施声明 |
P273: 避免释放到环境中。 P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P321: 特殊处理（请参阅此标签上的...）。 P405: 密闭存放 P501: 将内容物/容器处理到。。。 P264: 处理后要彻底洗手。 P260: 不要吸入灰尘/烟雾/气体/雾/蒸汽/喷雾。 P270: 使用本产品时，请勿进食、饮水或吸烟。 P391: 收集溢出物 P263: 避免在怀孕期间/哺乳期间接触。 P203: 使用前，获取、阅读并遵守所有安全说明。 P318: 如果暴露或担心，请就医。 P308+P316: 如果暴露或担心：立即寻求紧急医疗救助。 P319: 如果你感到不适，请寻求医疗帮助。 |
| Merck Index | 8270 |
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