Ro 48-8071 (CAS 161582-11-2)
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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 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
Ro 48-8071 (CAS 161582-11-2) References
1 Vance, D.E. Cholesterol and related derivatives. 2nd ed., 725-748 (1988). 2 Thoma, R., Schulz-Gasch, T., D'Arcy, 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. J Lipid Res 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. Mol Pharmacol 65 1302-1312 (2004).Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
Ro 48-8071, 5 mg | sc-205492 | 5 mg | $51.00 | |||
Ro 48-8071, 10 mg | sc-205492A | 10 mg | $128.00 |