Nevanimibe hydrochloride

Nevanimibe hydrochloride (PD-132301 hydrochloride) is an orally active and selective acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1) inhibitor with an EC50 of 9 nM. Nevanimibe hydrochloride inhibits ACAT2 with an EC50 of 368 nM. Nevanimibe hydrochloride induces cell apoptosis and has the potential for adrenocortical cancer.

Product information

CAS Number: 133825-81-7

Molecular Weight: 458.08

Formula: C27H40ClN3O

Synonym:

ATR101 hydrochloride

PD-132301 hydrochloride

Chemical Name: 1-[2, 6-bis(propan-2-yl)phenyl]-3-({1-[4-(dimethylamino)phenyl]cyclopentyl}methyl)urea hydrochloride

Smiles: Cl.CN(C)C1=CC=C(C=C1)C1(CNC(=O)NC2=C(C=CC=C2C(C)C)C(C)C)CCCC1

InChiKey: SDOOGTHIDFZUNM-UHFFFAOYSA-N

InChi: InChI=1S/C27H39N3O.ClH/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);1H

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 41.67 mg/mL (90.97 mM; Need ultrasonic)

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: ≥360 days 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 hydrochloride (PD-132301 hydrochloride; ATR101 hydrochloride; 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:

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.

Products are for research use only. Not for human use.