Rosuvastatin (Synonyms:瑞舒伐他汀;ZD 4522)
目录号 : KCM13149 CAS No. : 287714-41-4 纯度 : ≥98%
Rosuvastatin is an inhibitor of HMG-CoA reductase (IC = 5 nM). It inhibits cholesterol synthesis in isolated rat hepatocytes with an IC value of 0.16 nM. Rosuvastatin (10 mg/kg) reduces plasma total cholesterol, triglyceride, LDL-C, and oxidized LDL-C levels in Ldlr mice fed a high-fat diet. It decreases the area of aortic atherosclerotic lesions in the same model. Formulations containing rosuvastatin have been used in the treatment of dyslipidemias.
规格 价格 是否有货 数量
5mg
In-stock
10mg
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50mg
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100mg
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10 mM * 1 mL in DMSO
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生物活性

Rosuvastatin is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM. Rosuvastatin potently blocks hERG current with an IC50 of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels.

体内研究

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

Rosuvastatin (20 mg/kg/day, for 2 weeks) significantly reduces very low-density lipoproteins (VLDL) in diabetes mellitus rats induced by Streptozocin[2].

分子式
C22H28FN3O6S
分子量
481.54
CAS号
287714-41-4
中文名称
罗伐他汀;瑞舒伐他汀
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶解性数据
In Vitro:

DMSO : ≥ 100 mg/mL (207.67 mM)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0767 mL 10.3834 mL 20.7667 mL
5 mM 0.4153 mL 2.0767 mL 4.1533 mL
10 mM 0.2077 mL 1.0383 mL 2.0767 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂:10% DMSO → 40% PEG300 → 5% Tween-80 → 45% saline

    Solubility: ≥ 2.5 mg/mL (5.19 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.19 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

  • 2.

    请依序添加每种溶剂: 10% DMSO →  90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.19 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.19 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2