Powder: -20°C for 3 years | In solvent: -80°C for 1 year
A 922500 (DGAT-1 Inhibitor 4a) is an inhibitor for human and mouse DGAT-1 with IC50 of 7 nM and 24 nM, respectively, good selectivity over related acyltransferases, hERG, and a panel of anti-targets.
説明 | A 922500 (DGAT-1 Inhibitor 4a) is an inhibitor for human and mouse DGAT-1 with IC50 of 7 nM and 24 nM, respectively, good selectivity over related acyltransferases, hERG, and a panel of anti-targets. |
ターゲット&IC50 | DGAT-1 (mouse):24 nM, DGAT-1 (human):7 nM |
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] |
別名 | A922500, DGAT-1 Inhibitor 4a |
分子量 | 428.48 |
分子式 | C26H24N2O4 |
CAS No. | 959122-11-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 21.4 mg/mL (50 mM)
You can also refer to dose conversion for different animals. 詳細
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A 922500 959122-11-3 Metabolism Acyltransferase Transferase inhibit Inhibitor Diglyceride acyltransferase A922500 mono- acylglycerol acyltransferase acyl-CoA:cholesterol acyltransferase Diacylglycerol acyltransferase DGAT-1 Inhibitor 4a A-922500 inhibitor