Nevanimibe hydrochloride (Synonyms: PD-132301 hydrochloride; ATR101 hydrochloride) |
| カタログ番号GC65200 |
ネバニミブ塩酸塩 (PD-132301 塩酸塩) は、9 nM の EC50 を持つ経口活性で選択的なアシル補酵素 A: コレステロール O-アシルトランスフェラーゼ 1 (ACAT1) 阻害剤です。ネバニミブ塩酸塩は、368 nM の EC50 で ACAT2 を阻害します。ネバニミブ塩酸塩は細胞アポトーシスを誘導し、副腎皮質がんの可能性があります。
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Cas No.: 133825-81-7
Sample solution is provided at 25 µL, 10mM.
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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.
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