| 货号 | 10006415-5mg |
| 描述 | Oxidosqualene cyclase (OSC) is a microsomal enzyme that catalyzes the cyclization of monooxidosqualene to lanosterol in the cholesterol synthetic pathway.1,2 Ro 48-8071 is an inhibitor of oxidosqualene cyclase (OSC) that has low-density lipoprotein (LDL) cholesterol lowering activity similar to the 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) inhibitor simvastatin.3 It inhibits OSC from human liver microsomes and HepG2 cells with IC50 values of approximately 6.5 nM and 1.5 nM, respectively.3 Ro 48-8071 lowered LDL cholesterol ~40% in hamsters at a dose of 150 µg/kg without affecting high-density lipoprotein levels and with no sign of liver toxicity.3 Ro 48-8071 increases cytochrome P3A mRNA and protein levels in primary rat and murine hepatocyte cultures with a maximal effect at 30 µM.4 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Vance, D.E. Cholesterol and related derivatives. Biochemistry 2nd ed., 725-748 (1988). 2.Thoma, R.,Schulz-Gasch, T.,DArcy, B., et al. Insight into steroid scaffold formation from the structure of human oxidosqualene cyclase. Nature 432, 118-122 (2004). 3.Morand, O.H.,Aebi, J.D.,Dehmlow, H., et al. Ro 48-8071, a new 2,3-oxidosqualene:lanosterol cyclase inhibitor lowering plasma cholesterol in hamsters, squirrel monkeys, and minipigs: Comparison to simvastatin. Journal of Lipid Research 38, 373-390 (1997). 4.Shenoy, S.D.,Spencer, T.A.,Mercer-Haines, N.A., et al. Induction of CYP3A by 2,3-Oxidosqualene:Lanosterol cyclase inhibitors is mediated by an endogenouse squalene metabolite in primary cultured rat hepatocytes. Molecular Pharmacology 65, 1302-1312 (2004). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 448.4 |
| 分子式 | C23H27BrFNO2 |
| CAS号 | 161582-11-2 |
| 稳定性 | ≥ 1 year |
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