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Join us! · InformexUSA 2012 · New Orleans, Louisiana · February 14-17, 2012 · Booth 2514

Ro 48-8071

Cayman Chemical Item Number 10006415

(CAS 161582-11-2)

Ro 48-8071 (CAS 161582-11-2)

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Description

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 Hep-G2 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

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).

Formal Name (4-​bromophenyl)[2-​fluoro-​4-​[[6-​(methyl-​2-​propenylamino)hexyl]oxy]phenyl]-​methanone
CAS Number 161582-11-2
Molecular Formula C23H27BrFNO2
Formula Weight 448.4
Formulation A solution in methyl acetate
Purity >98%
Stability 1 year
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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C=CCN(C)​CCCCCCOc1ccc(c(F)​c1)​C(=O)​c1ccc(Br)​cc1

Background Reading

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).

Vance, D.E. Cholesterol and related derivatives. 2nd ed. 725-748 (1988).

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).

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).

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Ro 48-8071 is available in the following screening library:

Size Price Quantity Subtotal
5 mg $33.00 $0.00
10 mg $63.00 $0.00
50 mg $264.00 $0.00
100 mg $462.00 $0.00
Bulk Contact
Cart Total $0.00

This product is available in custom sizes and/or larger quantities.

Please contact our Sales Department for a quote or to purchase.

Pricing updated 2012-02-12. Prices are subject to change without notice.

To ask for assistance with one of our products please contact a Technical Support Scientist.

Warning This product is not for human or veterinary use.

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