133825-81-7

133825-81-7 structure

Name: Nevanimibe hydrochloride
Chemical Name: 1-[[1-[4-(dimethylamino)phenyl]cyclopentyl]methyl]-3-[2,6-di(propan-2-yl)phenyl]urea,hydrochloride
CAS Number: 133825-81-7
Molecular Formula: C₂₇H₄₀ClN₃O
Molecular Weight: 458.07900
Catalog: Signaling Pathways Metabolic Enzyme/Protease Acyltransferase
Create Date: 2017-05-10 17:23:27
Modify Date: 2024-01-02 11:01:38
Nevanimibe hydrochloride (PD-132301 hydrochloride; ATR101 hydrochloride) is a selective and potent acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1) inhibitor with an EC50 of 9 nM. Nevanimibe hydrochloride (PD-132301 hydrochloride; ATR101 hydrochloride) inhibits ACAT2 with an EC50 of 368 nM[1].

Name	1-[[1-[4-(dimethylamino)phenyl]cyclopentyl]methyl]-3-[2,6-di(propan-2-yl)phenyl]urea,hydrochloride
Synonyms	Urea,N-(2,6-bis(1-methylethyl)phenyl)-N'-((1-(4-(dimethylamino)phenyl)cyclopentyl)methyl)-,monohydrochloride C27H39N3O.HCl N-(2,6-Bis(1-methylethyl)phenyl)-N'-((1-(4-(dimethylamino)phenyl)cyclopentyl)methyl)urea HCl

Description	Nevanimibe hydrochloride (PD-132301 hydrochloride; ATR101 hydrochloride) is a selective and potent acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1) inhibitor with an EC50 of 9 nM. Nevanimibe hydrochloride (PD-132301 hydrochloride; ATR101 hydrochloride) inhibits ACAT2 with an EC50 of 368 nM[1].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Metabolic Enzyme/Protease >> Acyltransferase
Target	ACAT1:9 nM (EC50) ACAT2:368 nM (EC50)
In Vitro	Coincubation of Nevanimibe (ATR-101; 3 nM-30 μM) and Cholesterol markedly increases toxicity in a dose-dependent manner, where 3 nM Nevanimibe in the presence of 60 μg/mL Cholesterol reduces survival by 60% after 24 hours. All doses of Nevanimibe (3 nM-30 μM) induces cytoxicity in the presence of Cholesterol, whereas treatment with Cholesterol in the absence of Nevanimibe has no effect on cell viability[1]. Cell Cytotoxicity Assay[1] Cell Line: The H295R and HAC clone 15 (HAC15) human ACC cell lines Concentration: 3 nM-30 μM Incubation Time: 24 hours Result: 3 nM-3 μM exhibited no toxicity, whereas 30 μM treatment reduced survival by approximately 40% within 24 hours.
References	[1]. LaPensee CR, et al. ATR-101, a Selective and Potent Inhibitor of Acyl-CoA Acyltransferase 1, Induces Apoptosis in H295R Adrenocortical Cells and in the Adrenal Cortex of Dogs. Endocrinology. 2016 May;157(5):1775-88.