详情描述
Nevanimibe (PD-132301) is an orally active and selective acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1) inhibitor with an EC50 of 9 nM. Nevanimibe inhibits ACAT2 with an EC50 of 368 nM. Nevanimibe induces cell apoptosis and has the potential for adrenocortical cancer.
Product information
CAS Number: 133825-80-6
Molecular Weight: 421.62
Formula: C27H39N3O
Synonym:
PD-132301
ATR-101
Chemical Name: 1-[2, 6-bis(propan-2-yl)phenyl]-3-({1-[4-(dimethylamino)phenyl]cyclopentyl}methyl)urea
Smiles: CN(C)C1=CC=C(C=C1)C1(CNC(=O)NC2=C(C=CC=C2C(C)C)C(C)C)CCCC1
InChiKey: PKKNCEXEVUFFFI-UHFFFAOYSA-N
InChi: InChI=1S/C27H39N3O/c1-19(2)23-10-9-11-24(20(3)4)25(23)29-26(31)28-18-27(16-7-8-17-27)21-12-14-22(15-13-21)30(5)6/h9-15,19-20H,7-8,16-18H2,1-6H3,(H2,28,29,31)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
Coincubation of Nevanimibe (PD-132301; ATR101; 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.
References:
- 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.
Products are for research use only. Not for human use.