A potent oxidosqualene cyclase inhibitor with cholesterol lowering activity
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Ro 48-8071

Item No. 10006415

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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
Purity
≥95%
Formulation
A 50 mg/ml solution in methyl acetate
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 30 mg/mlEthanol:PBS (pH 7.2) (1:2): .25 mg/ml
SMILES
C=CCN(C)CCCCCCOc1ccc(c(F)c1)C(=O)c1ccc(Br)cc1
InChi Code
InChI=1S/C23H27BrFNO2/c1-3-14-26(2)15-6-4-5-7-16-28-20-12-13-21(22(25)17-20)23(27)18-8-10-19(24)11-9-18/h3,8-13,17H,1,4-7,14-16H2,2H3
InChi Key
CMYCCJYVZIMDFU-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $46

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    10 mg

    $86

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    50 mg

    $355

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    100 mg

    $618

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    Cayman Chemical
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    OBESITY RESEARCH SOLUTIONS
    Product Description

    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.1 It inhibits OSC from human liver microsomes and HepG2 cells with IC50 values of approximately 6.5 nM and 1.5 nM, respectively.1 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.1 Ro 48-8071 increases cytochrome P3A mRNA and protein levels in primary rat and murine hepatocyte cultures with a maximal effect at 30 µM.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. 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).

    2. 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).