Nevanimibe(Synonyms: PD-132301; ATR-101)

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Nevanimibe (Synonyms: PD-132301; ATR-101)

Nevanimibe (PD-132301) 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 抑制 ACAT2,EC50 为 368 nM。Nevanimibe 诱导细胞凋亡 (apoptosis),并具有抗肾上腺皮质癌的潜力。

Nevanimibe(Synonyms: PD-132301;  ATR-101)

Nevanimibe Chemical Structure

CAS No. : 133825-80-6

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Nevanimibe 的其他形式现货产品:

Nevanimibe hydrochloride

生物活性

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[1].

IC50 & Target

ACAT1

9 nM (EC50)

ACAT2

368 nM (EC50)

体外研究
(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[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Clinical Trial

分子量

421.62

Formula

C27H39N3O

CAS 号

133825-80-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [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.

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