An inhibitor of oxidosqualene cyclase (OSC) that has LDL cholesterol lowering activity; inhibits OSC from human liver microsomes and HepG2 cells with IC50 values of approximately 6.5 and 1.5 nM

Ro 48-8071 – 5 mg

Brand:
Cayman
CAS:
161582-11-2
Storage:
-20
UN-No:
De Minimis - 1231 / 3

Oxidosqualene cyclase (OSC) is a microsomal enzyme that catalyzes the cyclization of monooxidosqualene to lanosterol in the cholesterol synthetic pathway.{8343,12383} 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.{13141} It inhibits OSC from human liver microsomes and HepG2 cells with IC50 values of approximately 6.5 nM and 1.5 nM, respectively.{13141} 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.{13141} Ro 48-8071 increases cytochrome P3A mRNA and protein levels in primary rat and murine hepatocyte cultures with a maximal effect at 30 µM.{13142}  

 

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SKU: 10006415 - 5 mg Category:

Description

An inhibitor of oxidosqualene cyclase (OSC) that has LDL cholesterol lowering activity; inhibits OSC from human liver microsomes and HepG2 cells with IC50 values of approximately 6.5 and 1.5 nM, respectively

Formal name: (4-bromophenyl)[2-fluoro-4-[[6-(methyl-2-propenylamino)hexyl]oxy]phenyl]-methanone

Synonyms: 

Molecular weight: 448.4

CAS: 161582-11-2

Purity: ≥95%

Formulation: A solution in methyl acetate

Product Type|Biochemicals|Small Molecule Inhibitors|Sterol Biosynthesis||Research Area|Cardiovascular System|Lipids & Lipoproteins|Lipoproteins||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Dyslipidemias

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