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TUG-891 (CAS 1374516-07-0) LS-H131

GPR120 agonist
LS-H131-1 / 1 mg / $175
LS-H131-5 / 5 mg / $225
LS-H131-10 / 10 mg / $275
USA Shipment Only
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Description: GPR120 (free fatty acid receptor 4; FFAR4) is a G protein-coupled receptor (GPCR) expressed in intestine, adipocytes, and pro-inflammatory macrophages that is activated by long chain free fatty acids. ω-3 Fatty acids, such as docosahexaenoic acid and eicosapentaenoic acid, initiate GPR120 signaling resulting in inhibition of toll-like receptor and TNF- alpha inflammatory signaling pathways in a beta -arrestin2/TAB1 dependent manner. TUG-891 is a potent and selective agonist of GPR120 with pEC50 values of 7.36 and 7.77 for human and mouse GPR120, respectively. It activates GPR40 (FFAR1) with a pEC50 value of 4.19 and shows no activity at GPR41 (FFAR3) or GPR43 (FFAR2). H131_ChemicalStructureImage.png
4-[(4-fluoro-4'-methyl[1,1'-biphenyl]-2-yl)methoxy]-benzenepropanoic acid
 
biochemical, chemical, agonist
LS-H131
1374516-07-0
C23H21FO3
≥98%
A crystalline solid
0
CC1=CC=C(C2=CC=C(F)C=C2COC3=CC=C(CCC(O)=O)C=C3)C=C1
InChI=1S/C23H21FO3/c1-16-2-7-18(8-3-16)22-12-9-20(24)14-19(22)15-27-21-10-4-17(5-11-21)6-13-23(25)26/h2-5,7-12,14H,6,13,15H2,1H3,(H,25,26)
LPGBXHWIQNZEJB-UHFFFAOYSA-N
Shipped Ambient, store at -20°C, ≥ 2 years shelf life.
This product is for research use only. Not for administration to humans, or for human or veterinary diagnostic or therapeutic use.
Data Sheet DataSheet    SDS SDS
Related Products: O3FAR1 / GPR120 related products

Usage Information

TUG-891 is supplied as a crystalline solid. A stock solution may be made by dissolving the TUG-891 in the solvent of choice. TUG-891 is soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide (DMF), which should be purged with an inert gas. The solubility of TUG-891 in ethanol and DMF is approximately 1 mg/ml and approximately 10 mg/ml in DMSO. TUG-891 is sparingly soluble in aqueous buffers. For maximum solubility in aqueous buffers, TUG-891 should first be dissolved in DMSO and then diluted with the aqueous buffer of choice. TUG-891 has a solubility of approximately 0.1 mg/ml in a 1:5 solution of DMSO:PBS (pH 7.2) using this method. We do not recommend storing the aqueous solution for more than one day.

References:
  1. Davenport, A.P., Alexander, S.P.H., Sharman, J.L., et al. International Union of Basic and Clinical Pharmacology. LXXXVIII. G protein-coupled receptor list: Recommendations for new pairings with cognate ligands. Pharmacol. Rev. 65(3), 967-986 (2013).
  2. Oh, D.Y., Talukdar, S., Bae, E.J., et al. GPR120 is an omega-3 fatty acid receptor mediating potent anti-inflammatory and insulin sensitizing effects. Cell 142(5), 687-698 (2010).
  3. Shimpukade, B., Hudson, B.D., Hovgaard, C.K., et al. Discovery of a potent and selective GPR120 agonist. J. Med. Chem 55, 4511-4515 (2012).

 


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