1. GPCR/G Protein
  2. Free Fatty Acid Receptor
  3. GSK137647A

GSK137647A  (Synonyms: GSK 137647)

Cat. No.: HY-19995 Purity: 99.88%
COA Handling Instructions

GSK137647A (GSK 137647) is a potent, selective free fatty acid receptor 4 (FFA4) agonist with pEC50 values of 6.3, 6.2, and 6.1 for human, mouse and rat FFA4, and pEC50 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.

For research use only. We do not sell to patients.

GSK137647A Chemical Structure

GSK137647A Chemical Structure

CAS No. : 349085-82-1

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Solution
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
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ready for reconstitution
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Estimated Time of Arrival: December 31
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5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 96 In-stock
Estimated Time of Arrival: December 31
25 mg USD 192 In-stock
Estimated Time of Arrival: December 31
50 mg USD 312 In-stock
Estimated Time of Arrival: December 31
100 mg USD 540 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE GSK137647A

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

GSK137647A (GSK 137647) is a potent, selective free fatty acid receptor 4 (FFA4) agonist with pEC50 values of 6.3, 6.2, and 6.1 for human, mouse and rat FFA4, and pEC50 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.
Molecular Weight

305.39

Formula

C16H19NO3S

CAS No.
SMILES

O=S(C1=CC=C(OC)C=C1)(NC2=C(C)C=C(C)C=C2C)=O

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
In Vitro: 

DMSO : ≥ 100 mg/mL (327.45 mM)

H2O : mg/mL (ultrasonic;warming) (Need ultrasonic and warming)

*"≥" means soluble, but saturation unknown.

Preparing
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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (8.19 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
GSK137647A
Cat. No.:
HY-19995
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