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A-922500 (DGAT-1 Inhibitor 4a) is a potent orally active inhibitor of DGAT-1 activity, inhibiting both human and mouse forms of the enzymes with IC50 values of 9 and 22 nM, respectively. 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 conferred significant weight loss within seven days without affecting food intake and significantly reduced plasma and liver triglycerides with chronic dosing when administered at 3 mg/kg to DIO mice. DGAT-1 inhibitor A-922500 (0.03, 0.3 and 3 mg/kg, p.o.), dose-dependently attenuated the maximal postprandial rise in serum triglyceride concentrations. A-922500 is devoid of activity at DGAT-2, ACAT1 or ACAT2.
| Molecular Weight | 428.48 |
| Formula | C26H24N2O4 |
| CAS Number | 959122-11-3 |
| Solubility (25°C) | DMSO 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related DGAT Products |
|---|
| AZD7687
AZD7687 is a reversible and selective DGAT1 inhibitor with IC50 value of 80 nM. |
| PF-04620110
PF-04620110 is an orally active, selective and potent diglyceride acyltransferase-1 (DGAT1) inhibitor with IC50 of 19 nM. |
| AZD 3988
AZD 3988 is a potent and selective DGAT-1 inhibitor. |
| PF-06424439 methanesulfonate
PF-06424439 methanesulfonate is a potent and selective inhibitor of diacylglycerol acyltransferase 2 (DGAT2) with an IC50 of 14 nM. |
| T863
T863 is an orally active, selective and potent DGAT1 (Acyl-CoA:diacylglycerol acyltransferase 1) inhibitor that interacts with the acyl-CoA binding site of DGAT1, and inhibits triacylglycerol synthesis in cells. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
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