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Purity: ≥98%
GSK137647A, a diarylsulfonamide analog, is a novel, potent and selective agonists of the free fatty acid receptor 4 (FFA4/GPR120) with pEC50 of 6.3, 6.2, and 6.1 for human, mouse and rat FFA4, respectively. GSK137647A prefers to target GPR120 above a panel of 61 other targets, which includes additional FFARs. The G protein-coupled receptor family contains the free fatty acid receptor 4 (FFA4/GPR120), a putative 7TM (transmembrane) receptor that is involved in the secretion of glucagon-like peptide-1 (GLP-1) in response to long-chain fatty acid stimulation. The intestinal endocrine cell line STC-1 and the intestine both exhibit high expression levels of FFA4.
| Targets |
GPR120
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|---|---|---|
| ln Vitro |
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| ln Vivo |
GSK137647A (GSK 137647) (1 mg/kg; i.p.; twice daily, for 7 days) reduces colitis in C57BL/6 mice given TNBS and DSS[1].
GSK137647A (GSK 137647) (1 mg/kg; i.p.; twice daily, for 7 days; C57BL/6 mice) increases intestinal permeability in vivo[1]. |
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| Cell Assay |
Cell Line: Caco-2 cells
Concentration: 30 µM Incubation Time: 12 hours Result: Downregulated FFAR1, FFAR2, and FFAR4 as compared to control. |
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| Animal Protocol |
Male C57BL/6 mice
1 mg/kg Intraperitoneal injection; twice daily, for 7 days |
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| References |
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| Molecular Formula |
C₁₆H₁₉NO₃S
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|---|---|---|
| Molecular Weight |
305.39
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| Exact Mass |
305.109
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| Elemental Analysis |
C, 62.93; H, 6.27; N, 4.59; O, 15.72; S, 10.50
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| CAS # |
349085-82-1
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| Related CAS # |
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| PubChem CID |
743974
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| Appearance |
White to off-white solid powder
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| LogP |
4.575
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
21
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| Complexity |
411
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S(C1C([H])=C([H])C(=C([H])C=1[H])OC([H])([H])[H])(N([H])C1C(C([H])([H])[H])=C([H])C(C([H])([H])[H])=C([H])C=1C([H])([H])[H])(=O)=O
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| InChi Key |
FQUAFMNPXPXOJE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H19NO3S/c1-11-9-12(2)16(13(3)10-11)17-21(18,19)15-7-5-14(20-4)6-8-15/h5-10,17H,1-4H3
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| Chemical Name |
4-methoxy-N-(2,4,6-trimethylphenyl)benzenesulfonamide
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.19 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2745 mL | 16.3725 mL | 32.7450 mL | |
| 5 mM | 0.6549 mL | 3.2745 mL | 6.5490 mL | |
| 10 mM | 0.3275 mL | 1.6373 mL | 3.2745 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Bioorg Med Chem Lett.2014 Jul 15;24(14):3100-3. |
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