GSK137647A

SKU: orb1223139

Description

GSK137647A is an agonist of the free fatty acid receptor 4 (FFA4/GPR120) with pEC50s = 6.3, 6.2, and 6.1 at human, mouse, and rat receptors, respectively. GSK137647A is selective for GPR120 over a panel of 61 other targets, including other FFARs.

Key Properties

• CAS Number: 349085-82-1
• MW: 305.39
• Purity: >98% (HPLC)
• Formula: C₁₆H₁₉NO₃S
• SMILES: Cc1cc(c(c(c1)C)NS(=O)(=O)c1ccc(cc1)OC)C
• Target: AChR
• Solubility: DMSO : ≥ 32 mg/mL. 104.78 mM; H2O : < 0.1 mg/mL

Bioactivity

• 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. GSK137647A (GSK 137647) (1 mg/kg; i.p.; twice daily, for 7 days; C57BL/6 mice) restores intestinal permeability In vivo. Animal model: Male C57BL/6 mice. 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. Dosage: 1 mg/kg. Administration: Intraperitoneal injection; twice daily, for 7 days. Result: Decreased the amount of FITC and alleviated intestinal epithelial barrier permeability.
• In Vitro:
  GSK137647A (GSK 137647) (50 μM) reduces the production of NO in macrophages without affecting cell viability. GSK137647A (GSK 137647) (30 μM; 12 hours) alleviates response to inflammatory stimuli in Caco-2 cells and induces secretion of IL-6.GSK137647A (GSK 137647) (10 μM) reduces the ion flow and affects the colonic epithelial ion transport in healthy. GSK137647A (GSK 137647) (50 μM) increases glucose stimulated insulin secretion. Western blot analysis. Cell line: Caco-2 cells. Concentration: 30 μM. Incubation time: 12 hours. Result: Down regulated FFAR1, FFAR2, and FFAR4 as compared to control. Cell Viability Assay Cell line: RAW264.7 macrophages Concentration: 10, 20 and 50 μM. Incubation time: 24 hours. Result: Without affected cell viability.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

GSK137647A | GSK-137647A

Quick Database Links

Gene Symbol

AChR