| 货号 | 10010338-5mg |
| 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 Lovastatin is an HMG-CoA reductase inhibitor that was initially isolated from Aspergillus terreus.2 Marketed as Mevinolin™, Mevacor™, and under several other trade names, Lovastatin was the first HMG-CoA reductase inhibitor to be used in the treatment of hypercholesterolemia. It is a competitive inhibitor of HMG-CoA reductase with a Ki value of 0.6 nM for the open ring, hydroxy acid form of the molecule.3 During a three week study in dogs, a dose of 8 mg/kg per day resulted in a 29% reduction in plasma cholesterol.3 Lovastatin also suppresses TNF-induced NF-κB activation (IC50 ~ 15 µM), which potentiates apoptosis in human myeloid leukemia cells and thus, maybe useful in treating cancer.4 |
| 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.Endo, A. The discovery and development of HMG-CoA reductase inhibitors. Journal of Lipid Research 33, 1569-1582 (1992). 3.Alberts, A.W.,Chen, J.,Kuron, G., et al. Mevinolin: A highly potent competitive inhibitor of hydroxymethylglutaryl-coenzyme A reductase and a cholesterol-lowering agent. Proceedings of the National Academy of Sciences of the United States of America 77(7), 3957-3961 (1980). 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 | 404.5 |
| 分子式 | C24H36O5 |
| CAS号 | 75330-75-5 |
| 稳定性 | ≥ 2 years |
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