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Diacylglycerol acyltransferase 1 (DGAT-1) inhibitor (IC50 values are 7 and 24 nM at human and mouse DGAT-1 respectively) that is devoid of activity at DGAT-2, ACAT1 or ACAT2. Induces significant weight loss without altering food intake, and decreases liver and plasma triglyceride levels in vivo. Orally active.
|Storage||Desiccate at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 428.48. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.5 mM||4.67 mL||23.34 mL||46.68 mL|
|2.5 mM||0.93 mL||4.67 mL||9.34 mL|
|5 mM||0.47 mL||2.33 mL||4.67 mL|
|25 mM||0.09 mL||0.47 mL||0.93 mL|
References are publications that support the biological activity of the product.
Zhao et al (2008) Validation of diacyl glycerolacyltransferase I as a novel target of obesity and dyslipidemia using a potent and selective small molecule inhibitor. J.Med.Chem. 51 380 PMID: 18183944
King et al (2009) Diacylglycerol acyltransferase 1 inhibition lowers serum triglycerides in the zucker fatty rat and the hyperlipidemic hamster. J.Pharmacol.Exp.Ther. 330 526 PMID: 19478132
King et al (2010) In vivo efficacy of acyl CoA: diacylglycerol acyltransferase (DGAT) 1 inhibition in rodent models of postprandial hyperlipidemia. Eur.J.Pharmacol. 637 155 PMID: 20385122
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Keywords: A 922500, A 922500 supplier, Diacylglycerol, acyltransferase, 1, DGAT-1, inhibitors, inhibits, Transferases, A922500, Inhibitor, 4a, O-Acyltransferase, 3587, Tocris Bioscience
4 Citations for A 922500
Citations are publications that use Tocris products. Selected citations for A 922500 include:
Camus et al (2013) Diacylglycerol acyltransferase-1 localizes hepatitis C virus NS5A protein to lipid droplets and enhances NS5A interaction with the viral capsid core. Nutr Metab (Lond) 288 9915 PMID: 23420847
Scott et al (2018) TFAP2 transcription factors are regulators of lipid droplet biogenesis. Elife 7 PMID: 30256193
Velliquette et al (2015) Identification of a botanical inhibitor of intestinal diacylglyceride acyltransferase 1 activity via in vitro screening and a parallel, randomized, blinded, placebo-controlled clinical trial. Cell Rep 12 27 PMID: 26246845
Poliakov et al (2012) Origin and evolution of retinoid isomerization machinery in vertebrate visual cycle: hint from jawless vertebrates. PLoS One 7 e49975 PMID: 23209628
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