RP 70676

• CAT Number: I013628
• CAS Number: 136609-26-2
• Molecular Formula: C25H28N4S
• Molecular Weight: 416.58
• Purity: ≥95%
• Synonyms: 1-[5-[(4,5-diphenyl-1H-imidazol-2-yl)sulfanyl]pentyl]-3,5-dimethylpyrazole
• InChI: InChI=1S/C25H28N4S/c1-19-18-20(2)29(28-19)16-10-5-11-17-30-25-26-23(21-12-6-3-7-13-21)24(27-25)22-14-8-4-9-15-22/h3-4,6-9,12-15,18H,5,10-11,16-17H2,1-2H3,(H,26,27)
• InChIKey: UUPITLNVYVCTFW-UHFFFAOYSA-N
• SMILES: CC1=CC(=NN1CCCCCSC2=NC(=C(N2)C3=CC=CC=C3)C4=CC=CC=C4)C

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].

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.