Nevanimibe hydrochloride

Nevanimibe hydrochloride (PD-132301 hydrochloride) 是选择性酰基辅酶 A：胆固醇 O-酰基转移酶 1 抑制剂，EC50为 9 nM。它抑制 ACAT2，EC50为 368 nM。它诱导细胞凋亡，具有抗肾上腺皮质癌的潜力。 体外活性： 在H295R人源肾上腺皮质癌细胞中，Nevanimibe hydrochloride(ATR-101 hydrochloride)能够降低胆固醇酯的形成并提升游离胆固醇(FC)水平，显示出对ACAT1活性的强效抑制。ATR-101处理还导致Caspase-3/7水平上升和末端脱氧核糖核酸转移酶2'-脱氧尿苷5'-三磷酸镍末端标记阳性细胞增加，这表明激活了细胞凋亡。 Nevanimibe hydrochloride (PD-132301 hydrochloride) is an orally active and selective acyl-coenzyme A:cholesterol O-acyltransferase 1 ( ACAT1 ) inhibitor with an EC 50 of 9 nM. Nevanimibe hydrochloride inhibits ACAT2 with an EC 50 of 368 nM. Nevanimibe hydrochloride induces cell apoptosis and has the potential for adrenocortical cancer 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Cytotoxicity AssayCell 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. IC50& Target:ACAT1 9 nM (EC 50 ) ACAT2 368 nM (EC 50 )

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