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Pravastatin Sodium

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Chemical Structure| 81131-70-6 同义名 : CS-514 sodium;Pravastatin (sodium salt)
CAS号 : 81131-70-6
货号 : A128695
分子式 : C23H35NaO7
纯度 : 98%
分子量 : 446.51
MDL号 : MFCD00887601
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(235.16 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 50 mg/mL(111.98 mM)
动物实验配方：
生物活性
描述 HMG-CoA reductase, the rate-limiting enzyme in the process of cholesterol synthesis in liver cells, catalyzes the production of mevalonate. Inhibiting HMG-CoA reductase inhibits cholesterol synthesis [3].Pravastatin sodium is an HMG-CoA reductase inhibitor that inhibits sterol synthesis with IC50 value of 5.6 μM[2]. In vitro, in animals and humans , it reduces plasma levels of LDL by inhibiting the synthesis of intracellular cholesterol. Among the three types of macrophages, including J-774 A.1 macrophage-like cells, human monocyte derived macrophages (HMDM) and mouse peritoneal macrophages (MPM), pravastatin sodium reduced intracellular cholesterol synthesis with IC50 of 0.08, 6.3 and 7.8 μg/ml, respectively[4]. Pravastatin sodium also moderates the individual aortic ring, with a maximum blood vessel dilation of 62.8% at 10 μM for 8 minutes. In cultured bovine arterial endothelial cells, Pravastatin sodium (< 10 μM) stimulates NOS activity and releases NO within 10 min, while L-arginine responds to pravastatin sodium (< 10 μM) by enhancing NO production[1]. In vivo, pravastatin (30 mg/kg/day) reduced malnutrition by 34%. In irradiated female wistar rats, CCN2 levels were reduced and Pravastatin (30 mg/kg/day) restored muscle structure[5]. In addition, Pravastatin (40 mg, single dose) reduced cholesterol synthesis rate by 62% in human monocyte derived macrophages and by 47% in patients with high cholesterol. Treatment of patients with elevated serum cholesterol with pravastatin at 40 mg per day for 8 weeks inhibited cholesterol synthesis by 55% and increased LDL degradation by 57%[4].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00982189 HIV Infection ... 展开 >> Cardiovascular Disease Risk 收起 << Not Applicable Completed - United States, Minnesota ... 展开 >> Hennepin County Medical Center Minneapolis, Minnesota, United States, 55415 收起 <<
NCT01857921 Coronary Artery Not Applicable Unknown October 2016 Korea, Republic of ... 展开 >> Severance Hospital Recruiting Seoul, Korea, Republic of, 120-752 Contact: Myeong Ki Hong, MD, PhD    82-2-2228-8460    mkhong61@yuhs.ac 收起 <<
NCT00697203 Dyslipidemia Phase 2 Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.24mL

0.45mL

0.22mL

11.20mL

2.24mL

1.12mL

22.40mL

4.48mL

2.24mL
参考文献

[3]The discovery and development of HMG-CoA reductase inhibitors