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Rosuvastatin Calcium
本半岛bd体育手机客户端 不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Rosuvastatin Calcium图片
CAS NO: 147098-20-2
包装与价格:
包装 价格(元)
10mM (in 1mL DMSO) 电议
10mg 电议
50mg 电议
100mg 电议
200mg 电议

半岛bd体育手机客户端 介绍
Rosuvastatin Calcium是一种竞争性HMG-CoA reductase抑制剂,无细胞试验中IC50为11 nM。
Cas No. 147098-20-2
别名 瑞舒伐他汀钙; Rosuvastatin hemicalcium; ZD 4522 Calcium
化学名 calcium;(E,3R,5S)-7-[4-(4-fluorophenyl)-2-[methyl(methylsulfonyl)amino]-6-propan-2-ylpyrimidin-5-yl]-3,5-dihydroxyhept-6-enoate
Canonical SMILES CC(C)C1=NC(=NC(=C1C=CC(CC(CC(=O)[O-])O)O)C2=CC=C(C=C2)F)N(C)S(=O)(=O)C.CC(C)C1=NC(=NC(=C1C=CC(CC(CC(=O)[O-])O)O)C2=CC=C(C=C2)F)N(C)S(=O)(=O)C.[Ca+2]
分子式 C44H54F2N6O12S2Ca
分子量 1001.14
溶解度 ≥ 28.55mg/mL in DMSO
储存条件 Store at 2-8℃
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
半岛bd体育手机客户端 描述

Rosuvastatin Calcium (Rosuvastatin hemicalcium) is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM[1]. Rosuvastatin Calcium potently blocks human ether-a-go-go related gene (hERG) current with an IC50 of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals[2]. Rosuvastatin Calcium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Calcium is very effective in lowering low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels[3].

Rosuvastatin Calcium (10 mg/kg, intraperitoneal) prolonges QTc in conscious and unrestraines guinea pigs from 201 ± 1 to 210 ± 2 ms.

References:
[1]. Watanabe, M., et al., Synthesis and biological activity of methanesulfonamide pyrimidine- and N-methanesulfonyl pyrrole-substituted 3,5-dihydroxy-6-heptenoates, a novel series of HMG-CoA reductase inhibitors. Bioorg Med Chem, 1997. 5(2): p. 437-44.
[2]. Carswell C.I., et al. Rosuvastatin. Drugs, 2002. 62(14): p. 2075-85; discussion 2086-7.
[3]. Plante I, et al. Rosuvastatin blocks hERG current and prolongs cardiac repolarization. J Pharm Sci. 2012 Feb;101(2):868-78.
[4]. Feng PF, et al. Intracellular Mechanism of Rosuvastatin-Induced Decrease in Mature hERG Protein Expression on Membrane. Mol Pharm. 2019 Apr 1;16(4):1477-1488.

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