货号 | 10010344-5mg |
描述 | Hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase is the rate-limiting enzyme in the cholesterol biosynthetic pathway and the target of the “statin” class of cholesterol-lowering drugs.1 Simvastatin is a competitive inhibitor of HMG-CoA reductase with a Ki value of 0.12 nM for the hydrolyzed, open ring form of the molecule.2 Simvastatin is marketed under the trade name Zocor™ and is often prescribed in combination with ezetimibe (Zetia) to treat dyslipidemia. This drug combination is known commercially as Vytorin™ or Inegy™. After 18 days of treatment with simvastatin in dogs at a dose of 8 mg/kg per day, plasma cholesterol levels were reduced by 33%.3 Simvastatin also suppresses TNF-induced NF-κB activation (IC50 ~ 13 µM), which potentiates apoptosis in human myeloid leukemia cells and thus may be useful in treating cancer.4 |
别名 | MK-733; |
供应商 | Cayman |
应用文献 | |
1.Tobert, J.A. Lovastatin and beyond: The history of the HMG-CoA reductase inhibitors. Nature Reviews.Drug Discovery 2(7), 517-526 (2003). 2.Corsini, A.,Maggi, F.M. and Catapano, A.L. Pharmacology of competitive inhibitors of HMG-CoA reductase. Pharmacological Research 31(1), 9-27 (1995). 3.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(Suppl 1), S11-S14 (1991). 4.Ahn, K.S.,Sethi, G. and Aggarwal, B.B. Reversal of chemoresistance and enhancement of apoptosis by statins through down-regulation of the NF-κB pathway. Biochemical Pharmacology 75(4), 907-913 (2008). | |
运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥98% |
计算分子量 | 418.6 |
分子式 | C25H38O5 |
CAS号 | 79902-63-9 |
稳定性 | ≥ 2 years |
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