ATR-101

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

ATR-101 (PD-132301, Nevanimibe) 是一种选择性有效的 ACAT1 抑制剂，IC50 为 52 nM。

ATR-101 (PD-132301, Nevanimibe) is a selective and potent inhibitor of ACAT1 with IC50 of 52 nM; induces H295R cell apoptosis, causes mitochondrial hyperpolarization, reactive oxygen release, and ATP depletion, caspase-3/7 activation, and membrane permeabilization; decreases the formation of cholesteryl esters and increases FC levels in H295R adrenocortical carcinoma cells; inhibits the establishment and impeds the growth of ACC-derived H295R cell xenografts in mice; orally active.Cushing Disease Phase 2 Clinical(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.

Cell Cytotoxicity Assay 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.

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PD-132301 | PD132301-2 | ATR 101 | Nevanimibe

Others

Other Targets

Other Targets

Endocrinology

Cushing Disease

133825-81-7

458.09

C27H40ClN3O

>98% (HPLC)

DMSO : 41.67 mg/mL. 90.97 mM

CC(C)C1=C(C(=CC=C1)C(C)C)NC(=O)NCC2(CCCC2)C3=CC=C(C=C3)N(C)C.Cl

1-(2,6-diisopropylphenyl)-3-((1-(4-(dimethylamino)phenyl)cyclopentyl)methyl)urea hydrochloride

(-20℃)

With Ice Pack

≥ 2 years