Ro 48-<wbr/>8071

Ro 48-8071

CAT N°: 10006415
Price:

From 62.00 52.70

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}

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • (4-bromophenyl)[2-fluoro-4-[[6-(methyl-2-propenylamino)hexyl]oxy]phenyl]-methanone
  • Correlated keywords
    • monooxidosqualenes cyclases inhibitors OSC cholesterols lowering activity microsomal enzymes catalyzes lanosterol synthetic pathway LDL low-density lipoproteins human livers microsomes HepG2 cells HDL high-desity toxicity CYP3A mRNA proteins hepatocytes cultures atherosclerosis
  • Product Overview:
    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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