货号:A128695 同义名: CS-514 sodium;Pravastatin (sodium salt)
Pravastatin Sodium is a competitive HMG-CoA reductase inhibitor with IC50 value of 5.6 μM.
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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]. |
Dose | Marmosets: 0.03 mg/kg - 30 mg/kg[3] (p.o.) Rat: 10 mg/kg - 100 mg/kg[4] (p.o.) Mice: 200 mg/kg, 250 mg/kg[4] (p.o.) |
Administration | p.o. |
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 | - | - |
计算器 | ||||
存储液制备 | 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 |
CAS号 | 81131-70-6 |
分子式 | C23H35NaO7 |
分子量 | 446.51 |
别名 | CS-514 sodium;Pravastatin (sodium salt) |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Inert atmosphere,2-8°C |
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 |