A TGR5 agonist
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TGR5 Receptor Agonist

Item No. 16291

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-(2-chlorophenyl)-N-(4-chlorophenyl)-N,5-dimethyl-4-isoxazolecarboxamide
CAS Number
1197300-24-5
Molecular Formula
C18H14Cl2N2O2
Formula Weight
361.2
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 50 mg/mlDMSO: 50 mg/mlDMSO:PBS (pH 7.2) (1:4): 0.2 mg/mlEthanol: 30 mg/ml
SMILES
ClC1=C(C2=NOC(C)=C2C(N(C3=CC=C(Cl)C=C3)C)=O)C=CC=C1
InChi Code
InChI=1S/C18H14Cl2N2O2/c1-11-16(17(21-24-11)14-5-3-4-6-15(14)20)18(23)22(2)13-9-7-12(19)8-10-13/h3-10H,1-2H3
InChi Key
IGRCWJPBLWGNPX-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    10 mg

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    25 mg

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    Cayman Chemical
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    Product Description

    TGR5 receptor agonist is an agonist of the bile acid G protein-coupled receptor TGR5 (EC50s = 31.6-158.5 nM in cell-based assays).1 It stimulates cAMP formation in HEK293 cells expressing TGR5 (EC50 = 2.3 pM).2 TGR5 receptor agonist (1 mg/kg) increases glucagon-like peptide 1 (GLP-1) secretion and decreases glucose levels in the hepatic portal vein in dogs when administered in combination with glucose.1 It also inhibits the cytochrome P450 (CYP) isozymes CYP2C19 and CYP3A4 (IC50s = 316.2 and 1,259 nM, respectively).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Evans, K.A., Budzik, B.W., Ross, S.A., et al. Discovery of 3-aryl-4-isoxazolecarboxamides as TGR5 receptor agonists. J. Med. Chem. 52(24), 7962-7965 (2009).

    2. Jensen, D.D., Godfrey, C.B., Niklas, C., et al. The bile acid receptor TGR5 does not interact with β-arrestins or traffic to endosomes but transmits sustained signals from plasma membrane rafts. The Journal of Biological Chemisty 288(32), 22942-22960 (2013).