[CAS NO. 349085-82-1] GSK137647A
PRODUCTS SPECIFICATIONS [349085-82-1]
DESCRIPTION [349085-82-1]
Overview
| MDL | MFCD02007969 |
|---|---|
| Molecular Weight | 305.39 |
| Molecular Formula | C16H19NO3S |
| SMILES | O=S(C1=CC=C(OC)C=C1)(NC2=C(C)C=C(C)C=C2C)=O |
1 Publications Citing Use of MCE
Summary
GSK137647A (GSK 137647) is a potent, selective free fatty acid receptor 4 ( FFA4 ) agonist with pEC 50 values of 6.3, 6.2, and 6.1 for human, mouse and rat FFA4, and pEC 50 values < 4.5 for all three species for FFA1, FFA2, and FFA3, respectively. GSK137647A has anti-inflammatory activity. GSK137647A induces insulin secretion and inhibits epithelial ion transport, GSK137647A is related to regulation of glucose homeostasis and anti-inflammatory response [1] [2] .
In Vitro
GSK137647A (GSK 137647) (50 µM) reduces the production of NO in macrophages without affecting cell viability
[1]
.
GSK137647A (GSK 137647) (30 µM; 12 hours) alleviates response to inflammatory stimuli in Caco-2 cells and induces secretion of IL-6
[1]
.
GSK137647A (GSK 137647) (10 µM) reduces the ion flow and affects the colonic epithelial ion transport in healthy
[1]
.
GSK137647A (GSK 137647) (50 µM) increases glucose stimulated insulin secretion
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Western Blot Analysis [1]
| Cell Line: | Caco-2 cells |
| Concentration: | 30 µM |
| Incubation Time: | 12 hours |
| Result: | Downregulated FFAR1, FFAR2, and FFAR4 as compared to control. |
Cell Viability Assay [1]
| Cell Line: | RAW264.7 macrophages |
| Concentration: | 10, 20 and 50 µM |
| Incubation Time: | 24 hours |
| Result: | Without affected cell viability. |
In Vivo
GSK137647A (GSK 137647) (1 mg/kg; i.p.; twice daily, for 7 days; C57BL/6 mice) alleviates colitis in TNBS- and DSS-treated mice
[1]
.
GSK137647A (GSK 137647) (1 mg/kg; i.p.; twice daily, for 7 days; C57BL/6 mice) restores intestinal permeability in vivo
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Male C57BL/6 mice [1] |
| Dosage: | 1 mg/kg |
| Administration: | Intraperitoneal injection; twice daily, for 7 days |
| Result: | Had anti-inflammatory effect and reversed colonic injury induced by DSS. |
| Animal Model: | Male C57BL/6 mice [1] |
| Dosage: | 1 mg/kg |
| Administration: | Intraperitoneal injection; twice daily, for 7 days |
| Result: | Decreased the amount of FITC and alleviated intestinal epithelial barrier permeability. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 100 mg/mL ( 327.45 mM )
H 2 O : mg/mL (ultrasonic;warming) (Need ultrasonic and warming)
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 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 |
-
1.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (8.19 mM); Clear solution
References
- [1] Salaga M, et, al. Activation of Free Fatty Acid Receptor 4 Affects Intestinal Inflammation and Improves Colon Permeability in Mice. Nutrients. 2021 Aug 6;13(8):2716.
- [2] Sparks SM, et, al. Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120). Bioorg Med Chem Lett. 2014 Jul 15;24(14):3100-3.