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133825-80-6

133825-80-6 structure
133825-80-6 structure
  • Name: Nevanimibe
  • Chemical Name: 1-[[1-[4-[(dimethylamino)methyl]phenyl]cyclopentyl]methyl]-3-[2,6-di(propan-2-yl)phenyl]urea
  • CAS Number: 133825-80-6
  • Molecular Formula: C28H41N3O
  • Molecular Weight: 435.64500
  • Catalog: Signaling Pathways Metabolic Enzyme/Protease Acyltransferase
  • Create Date: 2017-04-19 12:08:12
  • Modify Date: 2024-04-05 18:44:46
  • Nevanimibe (PD-132301; ATR101) is a selective and potent acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1) inhibitor with an EC50 of 9 nM. Nevanimibe (PD-132301; ATR101) inhibits ACAT2 with an EC50 of 368 nM[1].

Name 1-[[1-[4-[(dimethylamino)methyl]phenyl]cyclopentyl]methyl]-3-[2,6-di(propan-2-yl)phenyl]urea
Synonyms 1-[[1-[4-(dimethylaminomethyl)phenyl]cyclopentyl]methyl]-3-[2,6-di(propan-2-yl)phenyl]urea
Urea,N-[2,6-bis(1-methylethyl)phenyl]-N'-[[1-[4-(dimethylamino)phenyl]cyclopentyl]methyl]
Description Nevanimibe (PD-132301; ATR101) is a selective and potent acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1) inhibitor with an EC50 of 9 nM. Nevanimibe (PD-132301; ATR101) 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.

Density 1.062g/cm3
Boiling Point 528.1ºC at 760mmHg
Molecular Formula C28H41N3O
Molecular Weight 435.64500
Flash Point 273.2ºC
Exact Mass 435.32500
PSA 47.86000
LogP 6.90590
Vapour Pressure 3.05E-11mmHg at 25°C
Index of Refraction 1.58
Storage condition 2-8℃