A 922500

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Cat.No. 3587 - A 922500 | C26H24N2O4 | CAS No. 959122-11-3
Description: Potent DGAT-1 inhibitor
Alternative Names: DGAT-1 Inhibitor 4a
Chemical Name: (1R,2R)-2-[[4'-[[Phenylamino)carbonyl]amino] [1,1'-biphenyl]-4-yl]carbonyl]cyclopentanecarboxylic acid
Purity: ≥98% (HPLC)
Datasheet
Citations (4)
Reviews
Literature

Biological Activity

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.

Compound Libraries

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Technical Data

M. Wt 428.48
Formula C26H24N2O4
Storage Desiccate at +4°C
Purity ≥98% (HPLC)
CAS Number 959122-11-3
PubChem ID 24768261
InChI Key BOZRFEQDOFSZBV-DHIUTWEWSA-N
Smiles O=[C@]([C@@H]3CCC[C@H]3[C@@](O)=O)C(C=C2)=CC=C2C1=CC=C(NC(NC4=CC=CC=C4)=O)C=C1

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 21.42 50

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

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

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:

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

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

Scott et al (2018) TFAP2 transcription factors are regulators of lipid droplet biogenesis. Elife 7 PMID: 30256193

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


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Literature in this Area

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