Overview

  • Product name

    TGR5 Receptor Agonist, TGR5 G-protein coupled receptor agonist
  • Description

    Potent, selective TGR5 G-protein coupled receptor agonist
  • Biological description

    Potent, selective TGR5 G-protein coupled receptor agonist (pEC50 = 6.8). Increases glucagon-like peptide-1 (GLP-1) secretion from primary intestinal cells. Cell-permeable. Active in vivo.
  • Purity

    > 99%
  • CAS Number

    1197300-24-5
  • Chemical structure

    Chemical Structure

Properties

  • Chemical name

    3-(2-Chlorophenyl)-N-(4-chlorophenyl)-N,5-dimethyl-4-isoxazolecarboxamide
  • Molecular weight

    361.23
  • Molecular formula

    C18H14Cl2N2O2
  • PubChem identifier

    44605616
  • Storage instructions

    Store at -20°C. Store under desiccating conditions. The product can be stored for up to 12 months.
  • Solubility overview

    Soluble in ethanol to 100 mM and in DMSO to 100 mM
  • Handling

    Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.

    Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.

  • SMILES

    CC1=C(C(=NO1)C2=CC=CC=C2Cl)C(=O)N(C)C3=CC=C(C=C3)Cl
  • Source

    Synthetic

  • Research areas

References

This product has been referenced in:

  • Alemi F  et al. The receptor TGR5 mediates the prokinetic actions of intestinal bile acids and is required for normal defecation in mice. Gastroenterology 144:145-54 (2013). Read more (PubMed: 23041323) »
  • Li T  et al. The G protein-coupled bile acid receptor, TGR5, stimulates gallbladder filling. Mol Endocrinol 25:1066-71 (2011). Read more (PubMed: 21454404) »
  • Rizzo G  et al. Functional characterization of the semisynthetic bile acid derivative INT-767, a dual farnesoid X receptor and TGR5 agonist. Mol Pharmacol 78:617-30 (2010). Read more (PubMed: 20631053) »
  • Evans KA  et al. Discovery of 3-aryl-4-isoxazolecarboxamides as TGR5 receptor agonists. J Med Chem 52:7962-5 (2009). Read more (PubMed: 19902954) »
See 1 Publication for this product

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