Nevanimibe hydrochloride

Modify Date: 2024-01-02 11:01:38

Nevanimibe hydrochloride Structure
Nevanimibe hydrochloride structure
Common Name Nevanimibe hydrochloride
CAS Number 133825-81-7 Molecular Weight 458.07900
Density N/A Boiling Point 528.1ºC at 760 mmHg
Molecular Formula C27H40ClN3O Melting Point N/A
MSDS N/A Flash Point 273.2ºC

 Use of Nevanimibe hydrochloride


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].

 Names

Name 1-[[1-[4-(dimethylamino)phenyl]cyclopentyl]methyl]-3-[2,6-di(propan-2-yl)phenyl]urea,hydrochloride
Synonym More Synonyms

 Nevanimibe hydrochloride Biological Activity

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
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.

 Chemical & Physical Properties

Boiling Point 528.1ºC at 760 mmHg
Molecular Formula C27H40ClN3O
Molecular Weight 458.07900
Flash Point 273.2ºC
Exact Mass 457.28600
PSA 47.86000
LogP 7.71230
Vapour Pressure 3.05E-11mmHg at 25°C
Storage condition 2-8℃

 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