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ATR-101
- PD132301-2 - Nevanimibe hydrochloride- Parent CAS: 133825-80-6
- Soluble in DMSO
- MF: C27H39N3O.HCl
- MW: 458.08
Description
ATR-101 is a potent, selective and orally efficacious acyl coenzyme A:cholesterol acyltransferase isoform 1 (ACAT1) inhibitor (IC50 value of 0.009 µM). ATR-101 potently lowers plasma total cholesterol in various animal models of hypercholesterolemia but is an adrenal toxicant. Furthermore, ATR-101 inhibits cholesterol efflux and cortisol secretion by ATP-binding cassette transporters, causing cytotoxic cholesterol accumulation in ACC cells.
More Information
| Parent CAS No. | 133825-80-6 |
|---|---|
| Chemical Name | 1-(2,6-Diisopropylphenyl)-3-((1-(4-(dimethylamino)phenyl)cyclopentyl)methyl)urea hydrochloride |
| SMILES | C1C=C(C(C)C)C(NC(NCC2(C3C=CC(N(C)C)=CC=3)CCCC2)=O)=C(C(C)C)C=1.Cl |
| MFCD | N.A. |
| InChi | InChI=1S/C27H39N3O.ClH/c1-19(2)23-10-9-11-24(20(3)4)25(23)29-26(31)28-18-27(16-7-8-17-27)21-12-14-22(15-13-21)30(5)6;/h9-15,19-20H,7-8,16-18H2,1-6H3,(H2,28,29,31);1H |
| InChiKey | SDOOGTHIDFZUNM-UHFFFAOYSA-N |
| CID | 131678 |
| Short Description | ACAT inhibitor |
References
- LA Vernetti et al. ATP depletion is associated with cytotoxicity of a novel lipid regulator in guinea pig adrenocortical cells. Toxicol Appl Pharmacol. 1993 Jan;118(1):30-8.
- BK Trivedi et al. Inhibitors of acyl-CoA:cholesterol acyltransferase (ACAT). 7. Development of a series of substituted N-phenyl-N'-[(1-phenylcyclopentyl)methyl]ureas with enhanced hypocholesterolemic activity. J Med Chem. 1994 May 27;37(11):1652-9.
- VE Burns et al. ATR-101 inhibits cholesterol efflux and cortisol secretion by ATP-binding cassette transporters, causing cytotoxic cholesterol accumulation in adrenocortical carcinoma cells. Br J Pharmacol. 2017 Oct;174(19):3315-3332.
- DK Langlois et al. ATR-101, a selective ACAT1 inhibitor, decreases ACTH-stimulated cortisol concentrations in dogs with naturally occurring Cushing's syndrome. BMC Endocr Disord. 2018 May 2;18(1):24.
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