Simvastatin (sodium salt)
(Synonyms: 辛伐他汀钠盐; Tenivastatin sodium; Simvastatin Impurity A sodium) 目录号 : GC12285
An HMG-CoA reductase inhibitor
Cas No.:101314-97-0
Sample solution is provided at 25 µL, 10mM.
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Ki: 0.12 nM
Simvastatin is a HMG-CoA reductase inhibitor.
HMG-CoA reductase has been found to be the rate-limiting enzyme in the cholesterol biosynthetic pathway and the target of the “statin” class of cholesterol-lowering drugs.
In vitro: Previous study found that simvastatin could inhibit the incorporation of 14C-acetate to 14C-sterol with an IC50 value of 15 nm in cultured Hep G2 cells. In addition, simvastatin was found to be a potent inhibitor of cholesterol synthesis in cultured liver cells, whereas pravastatin inhibited cholesterol synthesis in liver cells only after these cells had been digested by collagenase [1].
In vivo: Animal study showd that rats orally dosed with simvastatin had lower plasma cholesterol levels after 4 days of treatment. At the level of 0.02% of the diet, simvastatin lowered plasma cholesterol levels in rats by 64%. Moreove, in dogs, simvastatin at a daily oral dosage of 8 mg/kg lower levels of plasma cholesterol. At this dosage, simvastatin was slightly more potent than lovastatin and the levels of plasma cholesterol in these dogs returned to pretreatment levels after stopping the treatment [1].
Clinical trial: Previous clinical study found that both atorvastatin and simvastatin had significant PD reduction and RAL gain than placebo. Atorvastatin group showed greater mean PD reduction and mean RAL gain as compared to simvastatin group. Furthermore, atorvastatin group exhibited a significantly greater percentage of radiographic defect depth reduction as compared to simvastatin at 6 and 9 months [2].
References:
[1] Chao, Y. ,Chen, J.S.,Hunt, V.M., et al. Lowering of plasma cholesterol levels in animals by lovastatin and simvastatin. European Journal of Clinical Pharmacology 40, S11-S14 (1991).
[2] S Martande S, Kumari M, Pradeep AR, Pal Singh S, Kumar Suke D. nComparative evaluation of efficacy of subgingivally delivered 1.2% Atorvastatin and 1.2% Simvastatin in the treatment of intrabony defects in chronic periodontitis: a randomized controlled trial. J Dent Res Dent Clin Dent Prospects. 2017 Winter;11(1):18-25.
| Cas No. | 101314-97-0 | SDF | |
| 别名 | 辛伐他汀钠盐; Tenivastatin sodium; Simvastatin Impurity A sodium | ||
| 化学名 | (βR,δR,1S,2S,6R,8S,8aR)-8-(2,2-dimethyl-1-oxobutoxy)-1,2,6,7,8,8a-hexahydro-β,δ-dihydroxy-2,6-dimethyl-1-naphthaleneheptanoic acid, monosodium salt | ||
| Canonical SMILES | OC(/C=C/C=C\CCCCC)C/C=C\C/C=C\CCCC(O)=O | ||
| 分子式 | C25H39O6 • Na | 分子量 | 458.6 |
| 溶解度 | ≤10mg/ml in ethanol;10mg/ml in DMSO;10mg/ml in dimethyl formamide | 储存条件 | Store at RT |
| 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 | 2.1805 mL | 10.9027 mL | 21.8055 mL |
| 5 mM | 0.4361 mL | 2.1805 mL | 4.3611 mL |
| 10 mM | 0.2181 mL | 1.0903 mL | 2.1805 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