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ATR-101 free base

Chemical Structure : ATR-101 free base

CAS No.: 133825-80-6

ATR-101 free base (ATR101;Nevanimibe;PD-132301)

Catalog No.: PC-35460Not For Human Use, Lab Use Only.

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

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

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

Physicochemical Properties

M.Wt 421.629
Formula C27H39N3O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

References

1. LaPensee CR, et al. Endocrinology. 2016 May;157(5):1775-88.

2. Trivedi BK, et al. J Med Chem. 1994 May 27;37(11):1652-9.

3. Cheng Y, et al. Endocr Relat Cancer. 2016 Apr;23(4):1-19.

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