| Identification | Back Directory | [Name]
(4-BROMOPHENYL)[3-FLUORO-4-[[6-(METHYL-2-PROPENYLAMINO)HEXYL]OXY]PHENYL]-METHANONE | [CAS]
161582-11-2 | [Synonyms]
RO 48-8071
(4-Bromophenyl)[2-fluoro-4-[[6-(methyl-2-propenylamino)hexyl]oxy]phenyl]methanone
(4-BROMOPHENYL)[3-FLUORO-4-[[6-(METHYL-2-PROPENYLAMINO)HEXYL]OXY]PHENYL]-METHANONE
Methanone, (4-broMophenyl)[2-fluoro-4-[[6-(Methyl-2-propenylaMino)hexyl]oxy]phenyl]-
Methanone, (4-bromophenyl)[2-fluoro-4-[[6-(methyl-2-propen-1-ylamino)hexyl]oxy]phenyl]- | [Molecular Formula]
C23H27BrFNO2 | [MDL Number]
MFCD08062177 | [MOL File]
161582-11-2.mol | [Molecular Weight]
448.37 |
| Chemical Properties | Back Directory | [Boiling point ]
522.8±50.0 °C(Predicted) | [density ]
1.235±0.06 g/cm3(Predicted) | [storage temp. ]
Sealed in dry,2-8°C | [solubility ]
DMF: 30 mg/ml; DMSO: 30 mg/ml; Ethanol: 30 mg/ml; Ethanol:PBS (pH 7.2) (1:2): .25 mg/ml | [pka]
8.88±0.50(Predicted) |
| Hazard Information | Back Directory | [Description]
Oxidosqualene cyclase (OSC) is a microsomal enzyme that catalyzes the cyclization of monooxidosqualene to lanosterol in the cholesterol synthetic pathway. 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. It inhibits OSC from human liver microsomes and HepG2 cells with IC50 values of approximately 6.5 nM and 1.5 nM, respectively. 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. Ro 48-8071 increases cytochrome P3A mRNA and protein levels in primary rat and murine hepatocyte cultures with a maximal effect at 30 μM. | [Uses]
Ro 48-8071 is an inhibitor of oxidosqualene cyclase. | [Definition]
ChEBI: An aromatic ketone that is 2-fluoro-4'-bromobenzophenone in which the hydrogen at position 4 (meta to the fluoro group) is replaced by a 6-[methyl(prop-2-en-1-yl)amino]hexyl}oxy group. An inhibitor of lanosterol synthase. | [in vivo]
Ro 48-8071 lowers LDL-C maximally appr 60% at 150 μmol/kg per day, with no further reduction up to 300 μmol/kg per day, leaving HDL-C unchanged at all doses in hamsters. Ro 48-8071 (≥00 μmol/kg per day) increases the amount of MOS in liver of hamsters. Ro 48-8071 (300 μmol/kg per day) remarkedly and significantly reduces VLDL secretion of hamsters[1]. Ro 48-8071 (5 or 20 mg/kg) significantly reduces in vivo tumor growth in mice, without weight loss of the mice. Furthermore, Ro 48-8071 at a concentration of 20 mg/kg, completely eradicates two of the 12 tumors being monitored in the mice in the timeframe tested[2]. Ro 48-8071 (20 mg/day/kg body weight) leads to a rapid and sustained inhibition (>50%) of cholesterol synthesis in the whole small intestine of BALB/c mice. Sterol synthesis is also reduced in the large intestine and stomach[4]. |
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