product name A922500
Description: A922500 is a potent, selective and orally active inhibitor for human and mouse Acyl CoA/diacylglycerol acyltransferase (DGAT-1) with IC50 of 7 nM and 24 nM, respectively, good selectivity over related acyltransferases, hERG, and a panel of anti-targets. A 922500 confers weight loss and a reduction in liver triglycerides when dosed chronically in DIO mice and depletes serum triglycerides following a lipid challenge in a dose-dependent manner, thus, reproducing major phenotypical characteristics of DGAT-1(-/-) mice.
References: J Pharmacol Exp Ther. 2009;330:526-31; J Med Chem. 2008;51:380-3; Eur J Pharmacol. 2010;637:155-61.
428.48
Formula
C26H24N2O4
CAS No.
959122-11-3
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 86 mg/mL (200.7 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
15% Captisol: 20mg/mL
Synonyms
other peoduct :
| In Vitro |
In vitro activity: A 922500 inhibits the phylogenetic family members acyl coenzyme A cholesterol acyltransferase-1 and -2 with IC50 of 296 μM. A 922500 potently inhibits huDGAT-1 and mseDGAT-1. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Zucker fatty rats and diet-induced dyslipidemic hamsters are dosed orally with A 922500 (0.03, 0.3, and 3 mg/kg) for 14 days. Serum triglycerides ae significantly reduced by the 3 mg/kg dose of A 922500 in both the Zucker fatty rat (39%) and hyperlipidemic hamster (53%). These serum triglyceride changes are accompanied by significant reductions in free fatty acid levels by 32% in the Zucker fatty rat and 55% in the hyperlipidemic hamster. In addition, high-density lipoprotein-cholesterol is significantly increases (25%) in the Zucker fatty rat by A 922500 administered at 3 mg/kg. A 922500 confers weight loss and a reduction in liver triglycerides when dosed chronically in DIO mice and depletes serum triglycerides following a lipid challenge in a dose-dependent manner, thus, reproducing major phenotypical characteristics of DGAT-1(-/-) mice. A 922500 (0.03, 0.3 and 3 mg/kg, p.o.) dose-dependently attenuates the maximal postprandial rise in serum triglyceride concentrations. |
| Animal model | Male Golden Syrian hamsters with hyperlipidemia, and Male Zucker fatty rats |
| Formulation & Dosage | Dissolved in Polyethylene glycol/hydroxypropyl-β-cyclodextrin (10% w/v); 0.03, 0.3, and 3 mg/kg; oral gavage |
| References | J Pharmacol Exp Ther. 2009 Aug;330(2):526-31; J Med Chem. 2008 Feb 14;51(3):380-3; Eur J Pharmacol. 2010 Jul 10;637(1-3):155-61. |
