RP64477 Inhibitor

Solid. Powder

99.16%

Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent

498.72

DMSO: 8.33mg/mL (16.70mM) Need ultrasonic
(<1mg/ml refers to the product slightly soluble or insoluble)

C29H42N2O3S

CCCCCCCCCCOc1ccc(cc1)C(=O)Nc1cc(ccc1SC)C(=O)NCCCC

135239-65-5

ACAT

Inhibition by RP 64477 in a rabbit intestinal enzyme preparation was shown to be non-competitive with respect to the substrate oleoyl-CoA. In whole cell assays using human intestinal (CaCo-2), hepatic HepG2) and monocytic (THP-1) cell lines, RP 64477 inhibited ACAT activity with IC50s of 113, 503, and 180nM, respectively. RP 64477 (0.03% w/w by diet) reduced significantly cholesterol absorption in cholesterol/cholic acid-fed rats from 94+/- 8% to 65 +/- 4%. In cholesterol-fed rabbits, cholesterol absorption was reduced from 72 +/- 5% to 50 +/-5% and 44 +/- 5% at dose levels of 10 and 30 mg kg-1 b.i.d., respectively. Plasma cholesterol levels were reduced dose-dependently in both cholesterol/cholic-acid-fed rats and cholesterol-fed rabbits. Neither cholesterol absorption nor plasma cholesterol levels were reduced significantly in animals maintained on standard laboratory diets. Pharmacokinetic studies indicated that RP 64477 were very poorly absorbed following oral administration to rats.

ACAT; Others