A 922500

Pricing Availability Delivery Time Qty
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 (3)
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

A 922500 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

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.

All Tocris products are intended for laboratory research use only.

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 solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.33 mL 11.67 mL 23.34 mL
5 mM 0.47 mL 2.33 mL 4.67 mL
10 mM 0.23 mL 1.17 mL 2.33 mL
50 mM 0.05 mL 0.23 mL 0.47 mL

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

Product Datasheets

Certificate of Analysis / Product Datasheet
Select another batch:
Safety Datasheet

References

References are publications that support the products' biological activity.

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


If you know of a relevant reference for A 922500, please let us know.

View Related Products by Target

View Related Products by Product Action

View all Diacylglycerol O-Acyltransferase Inhibitors

Keywords: A 922500, supplier, Diacylglycerol, acyltransferase, 1, DGAT-1, inhibitors, inhibits, Transferases, A922500, DGAT-1, Inhibitor, 4a, Diacylglycerol, O-Acyltransferase, Diacylglycerol, O-Acyltransferase, Tocris Bioscience

3 Citations for A 922500

Citations are publications that use Tocris products. Selected citations for A 922500 include:

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

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

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


Do you know of a great paper that uses A 922500 from Tocris? If so please let us know.

Commented out for usability testing

Reviews

TODO: Add Reviews

Literature in this Area

New Product Guide

New Product Guide (Spring/Summer 2017)

Our new product guide highlights over 130 new products added to the Tocris Bioscience range during the first half of 2017.

  • 7-TM Receptors
  • Enzymes
  • Enzyme-Linked Receptors
  • Ion Channels
  • Nuclear Receptors
  • Transporters
  • Apoptosis
  • Cell Metabolism
  • Epigenetics
  • Fluorescent Imaging
  • Signal Transduction
  • Stem Cells

Pathways for A 922500

Protocols

TODO: Add Protocols