| Bioactivity | RP 70676 is a potent inhibitor of ACAT, with IC50 of 25 and 44 nM for rat and rabbit ACAT. | ||||||||||||
| Target | IC50: 25 nM (Rat ACAT), 44 nM (Rabbit ACAT) | ||||||||||||
| Invitro | 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. | ||||||||||||
| In Vivo | RP 70676 (10 mg/kg, p.o.) is well absorbed with plasma levels in NZW rabbits[1]. | ||||||||||||
| Name | RP 70676 | ||||||||||||
| CAS | 136609-26-2 | ||||||||||||
| Formula | C25H28N4S | ||||||||||||
| Molar Mass | 416.58 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
|
||||||||||||
| Reference | [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. |