Pravastatin sodium
(Synonyms: 普伐他汀钠; CS-514 sodium) 目录号 : GC14538
A potent HMG-CoA reductase inhibitor
Cas No.:81131-70-6
Sample solution is provided at 25 µL, 10mM.
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Pravastatin sodium is a high selective inhibitor of 3-hydroxy-3-methylglutaryl coenzyme-A (HMG-CoA) reductase of 44.1nM [1].
Pravastatin is a competitive inhibitor of HMG-CoA reductase. It has shown to reduce the level of plasma LDL both in animals and humans through inhibiting cellular cholesterol synthesis. Pravastatin was reported to reduce cellular cholesterol synthesis in three types of macrophages including J-774 A.1 macrophage-like cell line, human monocyte derived macrophages (HMDM) and mouse peritoneal macrophages (MPM) with IC50 values of 0.08, 6.3 and 7.8μg/ml, respectively [2].
Besides the benefit in cardiovascular disease prevention, pravastatin also has efficacy of preventing tumor growth in some degree. However, it has shown that the normal hepatocytes are more sensitive to pravastatin than the tumor cells since pravastatin is selectively taken up by OATP1B1 which is exclusively expressed in normal hepatocytes [3].
References:
[1] Bolego C, Poli A, Cignarella A, Catapano AL, Paoletti R. Novel statins: pharmacological and clinical results. Cardiovasc Drugs Ther. 2002 May;16(3):251-7.
[2] Keidar S, Aviram M, Maor I, Oiknine J, Brook JG. Pravastatin inhibits cellular cholesterol synthesis and increases low density lipoprotein receptor activity in macrophages: in vitro and in vivo studies. Br J Clin Pharmacol. 1994 Dec;38(6):513-9.
[3] Menter DG, Ramsauer VP, Harirforoosh S, Chakraborty K, Yang P, Hsi L, Newman RA, Krishnan K. Differential effects of pravastatin and simvastatin on the growth of tumor cells from different organ sites. PLoS One. 2011;6(12):e28813.
| Cell experiment [1]: | |
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Cell lines |
J-774 A.1 macrophage-like cells, human monocyte derived macrophages (HMDM) and mouse peritoneal macrophages (MPM) |
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Preparation method |
The solubility of this compound in DMSO is > 13.2 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
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Reacting condition |
0 ~ 100 μg/mL; 5 hrs |
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Applications |
In J-774 A.1 macrophage-like cells, HMDM and MPM, Pravastatin Sodium reduced cholesterol biosynthesis in a dose-dependent manner, with the IC50 values of 0.08 μg/mL, 6.3 μg/mL and 7.8 μg/mL, respectively. In J-774 A.1 macrophage-like cells, Pravastatin Sodium increased degradation of low density lipoprotein (LDL), but not degradation of acetyl LDL and oxidized LDL. |
| Animal experiment [2]: | |
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Animal models |
Otsuka Long-Evans Tokushima Fatty (OLETF) rats |
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Dosage form |
100 mg/kg/day; p.o.; for 8 weeks |
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Applications |
In OLETF rats, Pravastatin Sodium slightly reduced the fasting blood glucose level. However, Pravastatin Sodium significantly reduced superoxide production of vascular wall. In addition, Pravastatin Sodium normalized the level of serum glyceraldehyde-derived advanced glycation end-products (Glycer-AGEs). |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Keidar S, Aviram M, Maor I, Oiknine J, Brook JG. Pravastatin inhibits cellular cholesterol synthesis and increases low density lipoprotein receptor activity in macrophages: in vitro and in vivo studies. Br J Clin Pharmacol. 1994 Dec;38(6):513-9. [2]. Hori E, Kikuchi C, Nagami C, Kajikuri J, Itoh T, Takeuchi M, Matsunaga T. Role of Glyceraldehyde-derived AGEs and Mitochondria in Superoxide Production in Femoral Artery of OLETF Rat and Effects of Pravastatin. Biol Pharm Bull. 2017 Aug 22. |
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| Cas No. | 81131-70-6 | SDF | |
| 别名 | 普伐他汀钠; CS-514 sodium | ||
| 化学名 | sodium;(3R,5R)-3,5-dihydroxy-7-[(1S,2S,6S,8S)-6-hydroxy-2-methyl-8-[(2S)-2-methylbutanoyl]oxy-1,2,6,7,8,8a-hexahydronaphthalen-1-yl]heptanoate | ||
| Canonical SMILES | CCC(C)C(=O)OC1CC(C=C2C1C(C(C=C2)C)CCC(CC(CC(=O)[O-])O)O)O.[Na+] | ||
| 分子式 | C23H35O7.Na | 分子量 | 446.51 |
| 溶解度 | ≥ 13.15 mg/mL in DMSO, ≥ 100.4 mg/mL in EtOH with ultrasonic, ≥ 98.8 mg/mL in Water | 储存条件 | 4°C, protect from light |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2396 mL | 11.198 mL | 22.3959 mL |
| 5 mM | 0.4479 mL | 2.2396 mL | 4.4792 mL |
| 10 mM | 0.224 mL | 1.1198 mL | 2.2396 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet