GW9508
Based on 8 publication(s) in Google Scholar
GW9508 is a potent and selective G protein-coupled receptors FFA1 (GPR40) and GPR120 agonist with pEC50s of 7.32 and 5.46, respectively. GW9508 shows ~100-fold selectivity for GPR40 over GPR120. GW9508 is inactive against other GPCRs, kinases, proteases, integrins and PPARs. GW9508 is a glucose-sensitive insulin secretagogue and an ATP-sensitive potassium (KATP) channels opener. Anti-inflammatory and anti-atherosclerotic activities.
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- Pureza: 99.23%
- No. CAS: 885101-89-3
- Fòrmula: C22H21NO3
- Peso molecular:347.41
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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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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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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Publications Citing Use of MedChemExpress (MCE) GW9508
More- Cell Rep. 2024 Oct 10;43(10):114858. [Abstract]
- Biochem Pharmacol. 2025 May 1:116971. [Abstract]
- Am J Respir Cell Mol Biol. 2025 Jul 2. [Abstract]
- Inflammation. 2021 Apr;44(2):493-505. [Abstract]
- Int J Mol Sci. 2023 Mar 18;24(6):5801. [Abstract]
- Eur J Pharmacol. 2021 Oct 15:909:174362. [Abstract]
- Bioengineering (Basel). 2023 Apr 27;10(5):535. [Abstract]
- Curr Res Pharmacol Drug Discov. 2026 Jun 16:11:100260. [Abstract]
Customer Validation & Images
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Cell Imaging/Staining
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WB
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Histological Imaging/Staining
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ELISA
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Others
Actividad biológica
pEC50: 7.32 (GPR40) and 5.46 (GPR120)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
13 nM
Compound: GW 9508
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Agonist activity at human GPR40 expressed in CHO cells by calcium flux assay
Agonist activity at human GPR40 expressed in CHO cells by calcium flux assay
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[PMID: 24835985] |
| CHO | EC50 |
99 nM
Compound: GW 9508
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Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assay
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[PMID: 24835985] |
| HEK293 | EC50 |
>30 μM
Compound: 2, GW-9508
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Agonist activity at human GPR40 H137A mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calcium
Agonist activity at human GPR40 H137A mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calcium
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[PMID: 17552505] |
| HEK293 | EC50 |
1.2 μM
Compound: 2, GW-9508
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Agonist activity at human GPR40 H86F mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calcium
Agonist activity at human GPR40 H86F mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calcium
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[PMID: 17552505] |
| HEK293 | EC50 |
17.8 μM
Compound: 2, GW-9508
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Agonist activity at human GPR40 N244A mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calcium
Agonist activity at human GPR40 N244A mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calcium
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[PMID: 17552505] |
| HEK293 | EC50 |
2.2 μM
Compound: 2, GW-9508
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Agonist activity at human GPR40 H86A mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calcium
Agonist activity at human GPR40 H86A mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calcium
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[PMID: 17552505] |
| HEK293 | EC50 |
6.8 μM
Compound: 2, GW-9508
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Agonist activity at human GPR40 H137F mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calcium
Agonist activity at human GPR40 H137F mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calcium
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[PMID: 17552505] |
GW9508 stimulates intracellular Ca2+ mobilization in HEK-293 cells expressing GPR40 (pEC50 of 7.32) or GPR120 (pEC50 of 5.46), but not in the parent HEK-293 cell line[1].
GW9508 produces a concentration-dependent increase (pEC50 of 6.14) in glucose-stimulated insulin secretion at high glucose levels (25 mM). This resulted in a 1.52-fold increase in insulin secretion with 20 μM GW9508 in the presence of 25 mM glucose, compared with 25 mM glucose alone. The ability of GW9508 (10 μM) to enhance insulin secretion from MIN6 cells is significantly enhanced as glucose concentrations are increased[1].
GW9508 inhibits CCL17 and CCL5 expression in a pertussis toxin-sensitive manner. The inhibitory effect by GW9508 is abrogated by depletion of GPR40 with RNA interference. GW9508 further suppresses expression of IL-11, IL-24, and IL-33 induced in HaCaT cells by TNF-α and IFN-γ. GW9508 also inhibits CCL5 and CXCL10 production by normal human epidermal keratinocytes[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 885101-89-3
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Appearance Solid
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Peso molecular 347.41
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Fòrmula C22H21NO3
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Color White to off-white
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SMILES
O=C(O)CCC1=CC=C(NCC2=CC=CC(OC3=CC=CC=C3)=C2)C=C1
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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 (8)
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Journal Impact Factor
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Most Recent
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Cell Rep
Critical role of G protein-coupled receptor 40 in B cell response and the pathogenesis of rheumatoid arthritis in mice and patients. [Abstract]2024 Oct 10;43(10):114858. PMID: 39392754
GW9508 purchased from MedChemExpress. Usage Cited in: Cell Rep. 2024 Oct 10;43(10):114858. [Abstract]
GW9508 (100 μg). Representative images of hematoxylin-eosin (H&E), safranin O-fast green (S&F), and TRAP staining of forepaw ankle joint sections.
GW9508 purchased from MedChemExpress. Usage Cited in: Cell Rep. 2024 Oct 10;43(10):114858. [Abstract]
The levels of anti-collagen II IgM, IgG and IgA antibodies in the serum of mice treated with GW1100 and GW9508 (100 μg) after CIA induction.
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Biochem Pharmacol
GPR40 inhibits microglia-mediated neuroinflammation via the NLRP3/IL-1β/glutaminase pathway after subarachnoid hemorrhage. [Abstract]2025 May 1:116971. PMID: 40318813
GW9508 purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2025 May 1:116971. [Abstract]
Dihydroergotamine (DHE) staining was performed on the control group (ctr), GW9508 (10 μM; 12 h) group, GW9508 + GW1100 group, Hb group, Hb + GW9508 group, and Hb + GW9508 + GW1100 group. Scale bar = 20 μm. Arrows indicate the production of superoxide anions.
GW9508 purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2025 May 1:116971. [Abstract]
Representative Western blot plots of cleaved IL-1β and CD63 expression in the control group (ctr), GW9508 (10 μM; 12 h) group, GW9508 + GW1100 group, SAH group, SAH + GW9508 group and SAH + GW9508 + GW1100 group.
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Am J Respir Cell Mol Biol
2025 Jul 2. PMID: 40601883 -
Inflammation
GPR120 Ameliorates Apoptosis and Inhibits the Production of Inflammatory Cytokines in Renal Tubular Epithelial Cells. [Abstract]2021 Apr;44(2):493-505. PMID: 33009637 -
Int J Mol Sci
Adiponectin Enhances Fatty Acid Signaling in Human Taste Cells by Increasing Surface Expression of CD36. [Abstract]2023 Mar 18;24(6):5801. PMID: 36982874
GW9508 purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2023 Mar 18;24(6):5801. [Abstract]
Effect of AH-7614, AdipoRon, and AH-7614 + AdipoRon on calcium responses to 30 µM LA, and effect of AdipoRon on calcium responses to the GPR120 agonist GW9805 (10 µM).
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Eur J Pharmacol
GW9508 ameliorates cognitive dysfunction via the external treatment of encephalopathy in Aβ1-42 induced mouse model of Alzheimer's disease. [Abstract]2021 Oct 15:909:174362. PMID: 34297968 -
Bioengineering (Basel)
3D-Printed Bioactive Scaffold Loaded with GW9508 Promotes Critical-Size Bone Defect Repair by Regulating Intracellular Metabolism. [Abstract]2023 Apr 27;10(5):535. PMID: 37237605 -
Curr Res Pharmacol Drug Discov
Activation of G protein-coupled receptor 40 alleviates STAT6 activation, airway inflammation and mucus hypersecretion in allergic asthma. [Abstract]2026 Jun 16:11:100260. PMID: 42371471
Solvente y solubilidad
DMSO : ≥ 100 mg/mL (287.84 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.20 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.20 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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 (273 KB)
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SDS (620 KB)
- English - EN (620 KB)
- Français - FR (620 KB)
- Deutsch - DE (620 KB)
- Norwegian - NO (620 KB)
- Español - ES (620 KB)
- Swedish - SV (620 KB)
- Italian - IT (620 KB)
- Korean - KR (620 KB)
- Portuguese - PT (620 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Briscoe CP, et al. Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: identification of agonist and antagonist small molecules. Br J Pharmacol. 2006 Jul;148(5):619-28. [Content Brief]
[2]. Fujita T, et al. A GPR40 agonist GW9508 suppresses CCL5, CCL17, and CXCL10 induction in keratinocytes and attenuates cutaneous immune inflammation. J Invest Dermatol, 2011, 131(8), 1660-1667. [Content Brief]
[3]. Zhao YF, et al. Activation of ATP-sensitive potassium channels in rat pancreatic beta-cells by linoleic acid through both intracellular metabolites and membrane receptor signalling pathway. J Endocrinol, 2008, 198(3), 533-540. [Content Brief]
[4]. Suski M, et al. Anti-atherosclerotic action of GW9508 - Free fatty acid receptors activator - In apoE-knockout mice. Pharmacol Rep. 2019 Aug;71(4):551-555. [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 | 2.8784 mL | 14.3922 mL | 28.7844 mL | 71.9611 mL |
| 5 mM | 0.5757 mL | 2.8784 mL | 5.7569 mL | 14.3922 mL | |
| 10 mM | 0.2878 mL | 1.4392 mL | 2.8784 mL | 7.1961 mL | |
| 15 mM | 0.1919 mL | 0.9595 mL | 1.9190 mL | 4.7974 mL | |
| 20 mM | 0.1439 mL | 0.7196 mL | 1.4392 mL | 3.5981 mL | |
| 25 mM | 0.1151 mL | 0.5757 mL | 1.1514 mL | 2.8784 mL | |
| 30 mM | 0.0959 mL | 0.4797 mL | 0.9595 mL | 2.3987 mL | |
| 40 mM | 0.0720 mL | 0.3598 mL | 0.7196 mL | 1.7990 mL | |
| 50 mM | 0.0576 mL | 0.2878 mL | 0.5757 mL | 1.4392 mL | |
| 60 mM | 0.0480 mL | 0.2399 mL | 0.4797 mL | 1.1994 mL | |
| 80 mM | 0.0360 mL | 0.1799 mL | 0.3598 mL | 0.8995 mL | |
| 100 mM | 0.0288 mL | 0.1439 mL | 0.2878 mL | 0.7196 mL |
GW9508 Related Classifications
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