GSK137647A
Based on 1 publication(s) in Google Scholar
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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- Pureza: 99.81%
- No. CAS: 349085-82-1
- Fòrmula: C16H19NO3S
- Peso molecular:305.39
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) GSK137647A
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Actividad biológica
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.
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Cell Line:Caco-2 cells
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Concentration:30 µM
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Incubation Time:12 hours
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Result:Downregulated FFAR1, FFAR2, and FFAR4 as compared to control.
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Cell Line:RAW264.7 macrophages
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Concentration:10, 20 and 50 µM
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Incubation Time:24 hours
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Result:Without affected cell viability.
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.
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Animal Model:Male C57BL/6 mice[1]
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Dosage:1 mg/kg
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Administration:Intraperitoneal injection; twice daily, for 7 days
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Result:Had anti-inflammatory effect and reversed colonic injury induced by DSS.
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Animal Model:Male C57BL/6 mice[1]
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Dosage:1 mg/kg
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Administration:Intraperitoneal injection; twice daily, for 7 days
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Result:Decreased the amount of FITC and alleviated intestinal epithelial barrier permeability.
Chemical Information
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No. CAS 349085-82-1
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Appearance Solid
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Peso molecular 305.39
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Fòrmula C16H19NO3S
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Color White to off-white
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SMILES
O=S(C1=CC=C(OC)C=C1)(NC2=C(C)C=C(C)C=C2C)=O
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Synonyms
GSK 137647
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Front Immunol
Regulation of Free Fatty Acid Receptor 4 on Inflammatory Gene Induced by LPS in Large Yellow Croaker ( Larimichthys crocea). [Abstract]2021 Jun 10:12:703914. PMID: 34177969
Solvente y solubilidad
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.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureza y Documentación
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Ficha de datos (275 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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. [Content Brief]
[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. [Content Brief]
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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