RP64477 是有效的胆固醇酯化酶酰基辅酶 A：胆固醇 O-酰基转移酶 (ACAT) 抑制剂。

RP64477 is the cholesterol esterifying enzyme Acyl-coenzyme A:cholesterol O-acyltransferase (ACAT) inhibitor.

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 180 nM, 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.

135239-65-5

C29H42N2O3S

498.73

RP64477

DMSO:8.33 mg/mL (16.70 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years