| Name | A 922500 |
| Description | A 922500 (DGAT-1 Inhibitor 4a) is an inhibitor of human and mouse DGAT-1 with IC50 values of 7 nM and 24 nM, respectively, demonstrating good selectivity over related acyltransferases, hERG, and a panel of anti-targets. |
| In vitro | A 922500 inhibits the phylogenetic family members acyl coenzyme A cholesterol acyltransferase-1 and -2 with IC50 of 296 μM. [1] A 922500 potently inhibits huDGAT-1 and mseDGAT-1. [2] |
| 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. [1] 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. [2] A 922500 (0.03, 0.3 and 3 mg/kg, p.o.) dose-dependently attenuates the maximal postprandial rise in serum triglyceride concentrations. [3] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 70 mg/mL (163.37 mM), Sonication is recommended.
|
| Keywords | inhibit | Inhibitor | Acyltransferase | Diglyceride acyltransferase | A 922500 | mono- acylglycerol acyltransferase | acyl-CoA:cholesterol acyltransferase | Diacylglycerol acyltransferase | A-922500 |
| Inhibitors Related | Serotonin hydrochloride | Risedronate Sodium | Cyclandelate | Risedronic Acid | YM17E | 3-Methoxybenzamide | Entacapone | 2-Furoic acid | OU749 | Ibandronate sodium | Alendronate sodium hydrate | Flopropione |
| Related Compound Libraries | Bioactive Compound Library | Anti-Obesity Compound Library | Inhibitor Library | NO PAINS Compound Library | Lipid Metabolism Compound Library | Orally Active Compound Library | Metabolism Compound Library | Bioactive Compounds Library Max | Covalent Inhibitor Library |
United States
