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

GSK137647A  (Synonyms: GSK 137647)

Cat. No.: HY-19995 Purity: 99.81%
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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.

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GSK137647A Chemical Structure

GSK137647A Chemical Structure

CAS No. : 349085-82-1

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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Solution
10 mM * 1 mL in DMSO USD 66 In-stock
Solid
5 mg USD 60 In-stock
10 mg USD 96 In-stock
25 mg USD 192 In-stock
50 mg USD 312 In-stock
100 mg USD 540 In-stock
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Based on 1 publication(s) in Google Scholar

GSK137647A Related Antibodies

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

GSK137647A Related Antibodies

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].

MedChemExpress (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.
Appearance

Solid

Color

White to off-white

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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (327.45 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.2745 mL 16.3725 mL 32.7450 mL 81.8625 mL
5 mM 0.6549 mL 3.2745 mL 6.5490 mL 16.3725 mL
10 mM 0.3275 mL 1.6373 mL 3.2745 mL 8.1863 mL
15 mM 0.2183 mL 1.0915 mL 2.1830 mL 5.4575 mL
20 mM 0.1637 mL 0.8186 mL 1.6373 mL 4.0931 mL
25 mM 0.1310 mL 0.6549 mL 1.3098 mL 3.2745 mL
30 mM 0.1092 mL 0.5458 mL 1.0915 mL 2.7288 mL
40 mM 0.0819 mL 0.4093 mL 0.8186 mL 2.0466 mL
50 mM 0.0655 mL 0.3275 mL 0.6549 mL 1.6373 mL
60 mM 0.0546 mL 0.2729 mL 0.5458 mL 1.3644 mL
80 mM 0.0409 mL 0.2047 mL 0.4093 mL 1.0233 mL
100 mM 0.0327 mL 0.1637 mL 0.3275 mL 0.8186 mL
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GSK137647A Related Classifications

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.

Keywords:

GSK137647A349085-82-1GSK 137647GSK137647GSK-137647Free Fatty Acid ReceptorFFARFFA4FFA1FFA2FFA3insulin secretionepithelial ion transportanti-inflammatoryInhibitorinhibitorinhibit

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