136609-26-2

136609-26-2 structure

Name: RP 70676
Chemical Name: RP 70676
CAS Number: 136609-26-2
Molecular Formula: C₂₅H₂₈N₄S
Molecular Weight: 416.582
Catalog: Signaling Pathways Metabolic Enzyme/Protease Acyltransferase
Create Date: 2018-04-24 00:18:27
Modify Date: 2024-01-28 12:52:55
RP 70676 is a potent inhibitor of ACAT, with IC50 of 25 and 44 nM for rat and rabbit ACAT.

Name	RP 70676
Synonyms	1H-Pyrazole, 1-[5-[(4,5-diphenyl-1H-imidazol-2-yl)thio]pentyl]-3,5-dimethyl- 1-{5-[(4,5-Diphenyl-1H-imidazol-2-yl)sulfanyl]pentyl}-3,5-dimethyl-1H-pyrazole

Description	RP 70676 is a potent inhibitor of ACAT, with IC50 of 25 and 44 nM for rat and rabbit ACAT.
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> Acyltransferase Research Areas >> Metabolic Disease
Target	IC50: 25 nM (Rat ACAT), 44 nM (Rabbit ACAT)[1]
In Vitro	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].
References	[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.