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Products are for research use only. Not for human use. We do not sell to patients.
(DGAT-1 Inhibitor 4a; A-922500; A922500)
A 922500 Chemical Structure
|Product name: A 922500|
|Cat. No.: HY-10038|
A 922500 is a potent, selective, and orally bioavailable DGAT-1 inhibitor with IC50 values of 7 nM and 24 nM for human and mouse DGAT-1 respectively.
IC50 Value: 7 nM(human DGAT-1); 24 nM(DGAT-1) 
in vitro: A 922500 potently inhibits huDGAT-1 and mseDGAT-1 . A 922500 inhibits the phylogenetic family members acyl coenzyme A cholesterol acyltransferase-1 and -2 with IC50 of 296 μM .
in vivo: Zucker fatty rats and diet-induced dyslipidemic hamsters were dosed orally with A-922500 (0.03, 0.3, and 3-mg/kg), a potent and selective DGAT-1 inhibitor, for 14 days. Serum triglycerides were significantly reduced by the 3 mg/kg dose of the DGAT-1 inhibitor in both the Zucker fatty rat (39%) and hyperlipidemic hamster (53%) . 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 . The potent and selective DGAT-1 inhibitorA-922500 (0.03, 0.3 and 3 mg/kg, p.o.), dose-dependently attenuated the maximal postprandial rise in serum triglyceride concentrations in all species tested. At the highest dose of DGAT-1 inhibitor, the postprandial triglyceride response was abolished .
|M.Wt||428.48||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
10 mM in DMSO
|1 mg||5 mg||10 mg|
|1 mM||2.3338 mL||11.6692 mL||23.3383 mL|
|5 mM||0.4668 mL||2.3338 mL||4.6677 mL|
|10 mM||0.2334 mL||1.1669 mL||2.3338 mL|
. Zhao, Gang; Souers, Andrew J.; Validation of Diacyl Glycerolacyltransferase I as a Novel Target for the Treatment of Obesity and Dyslipidemia Using a Potent and Selective Small Molecule Inhibitor . Journal of Medicinal Chemistry (2008), 51(3), 380-383.
. King, Andrew J.; Segreti, Jason A.; Diacylglycerol acyltransferase 1 inhibition lowers serum triglycerides in the Zucker fatty rat and the hyperlipidemic hamster. Journal of Pharmacology and Experimental Therapeutics (2009), 330(2), 526-531.
. King AJ, Segreti JA, Larson KJ, Souers AJ, Kym PR, Reilly RM, Collins CA, Voorbach MJ, Zhao G, Mittelstadt SW, Cox BF.In vivo efficacy of acyl CoA: diacylglycerol acyltransferase (DGAT) 1 inhibition in rodent models of postprandial hyperlipidemia.Eur J Pharmacol. 2010 Jul 10;637(1-3):155-61. Epub 2010 Apr 10.
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