A potent inhibitor of DGAT-1 (IC50s = 7 and 24 nM

A-922500 – 1 mg

Brand:
Cayman
CAS:
959122-11-3
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

Diacylglycerol acyltransferases (DGATs) catalyze the final step in triglyceride synthesis. DGAT-1 deficient mice demonstrate a phenotype that is protective against the development of diet-induced obesity (DIO) or insulin resistance, implicating the actions of this enzyme in the development of such metabolic disorders. A-922500 is a potent orally active inhibitor of DGAT-1 activity, inhibiting both human and mouse forms of the enzymes with IC50 values of 7 and 24 nM, respectively.{15816} When administered at 3 mg/kg to DIO mice, A-922500 conferred significant weight loss within seven days without affecting food intake and significantly reduced plasma and liver triglycerides with chronic dosing.{15816} A-922500 does not inhibit DGAT-2, ACAT-1, or ACAT-2.{15816}  

 

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SKU: 10012708 - 1 mg Category:

Description

A potent inhibitor of DGAT-1 (IC50s = 7 and 24 nM, for human and mouse, respectively); confers significant weight loss within seven days and significantly reduces plasma and liver triglycerides when administered at 3 mg/kg to DIO mice

Formal name: 2R-[[4’-[[(phenylamino)carbonyl]amino][1R,1’-biphenyl]-4-yl-carbonyl]-cyclopentanecarboxylic acid

Synonyms:  (1R,2R)-2-(4′-(3-phenylureido)biphenylcarbonyl)-cyclopentanecarboxylic acid

Molecular weight: 428.5

CAS: 959122-11-3

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Acyltransferases||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Dyslipidemias||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Obesity

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