4-Methoxy-N-(2,4,6-triMethylphenyl)benzenesulfonaMide, 97% Chemical Properties

Boiling point:

438.1±55.0 °C(Predicted)

Density 

1.214±0.06 g/cm3(Predicted)

storage temp. 

2-8°C

solubility 

Soluble to 100 mM in DMSO and to 50 mM in ethanol.

form 

powder

pka

9.23±0.10(Predicted)

color 

white to beige

Stability:

Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 1 month.

CAS DataBase Reference

349085-82-1

4-Methoxy-N-(2,4,6-triMethylphenyl)benzenesulfonaMide, 97% Usage And Synthesis

Description

GSK-137647 (349085-82-1) is a potent and selective agonist at free fatty acid receptor 4 (FFA4), also known as GPR120. pEC50s= 6.3, 6.2 and 6.1 for human, mouse and rat receptor respectively.1 GSK-137647 enhances glucose-stimulated insulin secretion in mouse insulinoma cells and induces intracellular calcium increase in U2OS osteosarcoma cells expressing GPR120.2

Uses

4-Methoxy-N-(2,4,6-trimethylphenyl)benzenesulfonamide is involved in long-chain fatty acid stimulated GLP-1 secretion and has been implicated in glucose homeostasis, adiposity, and regulation of the anti-inflammatory response. It enhances glucose-stimulated insulin secretion in MIN6 cells. It induces intracellular calcium accumulation in U2OS cells; this activity is inhibited by AH 7614.

in vitro

gsk137647a (50 μm) induced a concentration-dependent increase in glucose (25 mm)-stimulated insulin secretion in min6 mouse insulinoma cell line [1]. in addition, gsk137647a (100 μm) induced a modest increase in glp-1 secretion in the human intestinal cell line nci-h716. moreover, gsk137647a induced intracellular calcium accumulation in u2os cells [1].

in vivo

gsk137647a (50 μm) induced active glp-1 release by mouse circumvallate papillae (cvps) [2].

target

ffa4/gpr120

storage

Store at RT

References

1) 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 2) Sparks?et al. (2014),?Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120); Bioorg. Med. Chem. Lett.,?24?3100

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