GSK 137647

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Cat.No. 5257 - GSK 137647 | C16H19NO3S | CAS No. 349085-82-1
Description: Potent and selective FFA4 (GPR120) agonist
Chemical Name: 4-Methoxy-N-(2,4,6-trimethylphenyl)benzenesulfonamide
Purity: ≥99% (HPLC)
Datasheet
Citations
Literature

Biological Activity

Potent and selective FFA4 (GPR120) agonist (pEC50 values are 6.3, 6.2 and 6.1 at the human, mouse and rat receptor, respectively). Exhibits ≥100-fold selectivity against a panel of 61 targets including FFA1, FFA2 and FFA3. Enhances glucose-stimulated insulin secretion in MIN6 cells. Induces intracellular calcium accumulation in U2OS cells; this activity is inhibited by AH 7614 (Cat. No. 5256).

Licensing Information

Sold for research purposes under agreement from GlaxoSmithKline

Compound Libraries

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Technical Data

M. Wt 305.39
Formula C16H19NO3S
Storage Store at RT
Purity ≥99% (HPLC)
CAS Number 349085-82-1
PubChem ID 743974
InChI Key FQUAFMNPXPXOJE-UHFFFAOYSA-N
Smiles CC1=CC(C)=CC(C)=C1NS(C2=CC=C(OC)C=C2)(=O)=O

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 30.54 100
ethanol 15.27 50

Preparing Stock Solutions

The following data is based on the product molecular weight 305.39. 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 3.27 mL 16.37 mL 32.75 mL
5 mM 0.65 mL 3.27 mL 6.55 mL
10 mM 0.33 mL 1.64 mL 3.27 mL
50 mM 0.07 mL 0.33 mL 0.65 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Sparks et al (2014) Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120). Bioorg.Med.Chem.Lett. 24 3100 PMID: 24881566

Martin et al (2012) Lipid-mediated release of GLP-1 by mouse taste buds from circumvallate papillae: putative involvement of GPR120 and impact on taste sensitivity. J.Lipid Res. 53 2256 PMID: 22904345


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Keywords: GSK137647 Free fatty acid receptor 4 diabetes potent and selective FFA4 GPR120 agonist Free Fatty Acid Receptors

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