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Nevanimibe hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Nevanimibe hydrochloride图片
CAS NO:133825-81-7
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议

产品介绍
Nevanimibe hydrochloride (PD-132301 hydrochloride) 是一种口服有效的,选择性酰基辅酶 A:胆固醇 O-酰基转移酶 1 (ACAT1) 抑制剂,EC50 为 9 nM。Nevanimibe hydrochloride 抑制 ACAT2,EC50 为 368 nM。Nevanimibe hydrochloride 诱导细胞凋亡 (apoptosis),并具有抗肾上腺皮质癌的潜力。
Cas No.133825-81-7
别名PD-132301 hydrochloride; ATR101 hydrochloride
分子式C27H40ClN3O
分子量458.08
溶解度DMSO : 41.67 mg/mL (90.97 mM; Need ultrasonic)|Water :< 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)
储存条件4°C, away from moisture
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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[1].

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[1].

[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.