ATR-101 free base

Research use only, not for human use.

ATR-101 (PD-132301, Nevanimibe) is a selective and potent inhibitor of ACAT1 with IC50 of 52 nM; induces H295R cell apoptosis.

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.

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. 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.

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ATR101 | Nevanimibe | PD-132301

Others

Other Targets

Other Targets

Endocrinology

Cushing Disease

133825-80-6

421.629

C27H39N3O

>98% (HPLC)

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O=C(NCC1(C2=CC=C(N(C)C)C=C2)CCCC1)NC3=C(C(C)C)C=CC=C3C(C)C

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

(-20℃)

With Ice Pack

≥ 2 years