| GSK 137647FFA4/GPR120 agonist |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
- View current batch:
- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
GSK 137647 Dilution Calculator
calculate
GSK 137647 Molarity Calculator
calculate
| Cas No. | 349085-82-1 | SDF | Download SDF |
| Chemical Name | N-mesityl-4-methoxybenzenesulfonamide | ||
| Canonical SMILES | CC1=CC(C)=C(NS(C2=CC=C(OC)C=C2)(=O)=O)C(C)=C1 | ||
| Formula | C16H19NO3S | M.Wt | 305.39 |
| Solubility | Soluble in DMSO | Storage | Store at RT |
| Physical Appearance | A crystalline solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
Target: FFA4/GPR120
IC50: N/A
GSK137647A is potent and selective FFA4/GPR120 agonist with pEC50 values of 6.3, 6.2, and 6.1 at the human, mouse and rat receptor, respectively [1]. The free fatty acid receptor 4 (FFA4/GPR120), a member of the G protein-coupled receptor family, is a potential 7TM receptor involved in long-chain fatty acid-stimulated glucagon-like peptide-1 (GLP-1) secretion. FFA4 is highly expressed in the intestinal endocrine cell line STC-1 and the intestine [1]. GLP-1 regulates multiple physiological functions including eating behavior [2].
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].
References:1. Sparks SM, Chen G, Collins JL, Danger D, Dock ST, Jayawickreme C, et al. Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120). Bioorg Med Chem Lett. 2014;24(14):3100-3. 2. Martin C, Passilly-Degrace P, Chevrot M, Ancel D, Sparks SM, Drucker DJ, et al. 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. 2012;53(11):2256-65.
