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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 |
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| PF-07202954
PF-07202954 is an orally active, weakly basic DGAT2 inhibitor with an IC50 of 10 nM for human DGAT2.PF-07202954 reduces hepatic triglycerides in an obese rat model. |
| ION224
ION224 is an antisense compound that targets DGAT-2 for studies related to non-alcoholic steatohepatitis (NASH). |
| PF-07055341
PF-07055341 is a DGAT1/2 inhibitor that can be used in studies related to non-alcoholic steatohepatitis (NASH). |
| Ervogastat
Ervogastat is a DGAT2 inhibitor that can be used in studies related to non-alcoholic steatohepatitis (NASH). |
| Pradigastat
Pradigastat (LCQ-908) is a potent, selective and orally active diacylglycerol acyltransferase 1 (DGAT1) inhibitor. Pradigastat has anti-obesity and anti-diabetic effects. |
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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