RP 70676 is a potent inhibitor of ACAT, with IC50 of 25 and 44 nM for rat and rabbit ACAT.
RP 70676 is a potent inhibitor of rabbit arterial ACAT (IC50 = 40 nM) and has been shown to be an effective inhibitor of ACAT derived from a number of tissues and species including man. The IC50 values range from 21 nM for hamster liver ACAT to 108 nM for enzyme from the intestine of cholesterol fed rabbits; in human hepatic tissues the mean IC50 is 44 nM. In whole cell P388D, murine macrophages the compound has an IC50 of 540 nM.
RP 70676 (10 mg/kg, p.o.) is well absorbed with plasma levels in NZW rabbits[1].
[1]. M.J. Ashton, et al. RP 70676: A potent systematically available inhibitor of acyl-CoA:cholesterol O-acyl transferase (ACAT). Bioorganic & Medicinal Chemistry Letters Volume 2, Issue 5, 1992, Pages 375-380.