Art. -Nr.: HY-15589

GW9508

8 Cited Publications

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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 (K_ATP) channels opener. Anti-inflammatory and anti-atherosclerotic activities.

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Reinheit: 99.23%
CAS. Nr.: 885101-89-3
Formel: C₂₂H₂₁NO₃
Molecular Weight:347.41

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

GW9508 Chemical Structure

CAS. Nr.: 885101-89-3

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (8)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

pEC50: 7.32 (GPR40) and 5.46 (GPR120)^[1]

Alle Free Fatty Acid Receptor Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	13 nM Compound: GW 9508	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	[PMID: 24835985]
CHO	EC₅₀	99 nM Compound: GW 9508	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	[PMID: 24835985]
HEK293	EC₅₀	>30 μM Compound: 2, GW-9508	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	[PMID: 17552505]
HEK293	EC₅₀	1.2 μM Compound: 2, GW-9508	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	[PMID: 17552505]
HEK293	EC₅₀	17.8 μM Compound: 2, GW-9508	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	[PMID: 17552505]
HEK293	EC₅₀	2.2 μM Compound: 2, GW-9508	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	[PMID: 17552505]
HEK293	EC₅₀	6.8 μM Compound: 2, GW-9508	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	[PMID: 17552505]

In Vitro

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.

In Vivo

Administration of GW9508 200 (μM) topically to the skin suppresses ear swelling in a repeated hapten application model (BALB/c and C57BL/6 mice) and contact hypersensitivity with downregulation of CCL5 and CXCL10, respectively^[2].

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

Chemical Information

CAS. Nr. 885101-89-3
Appearance Solid
Molecular Weight 347.41
Formel C₂₂H₂₁NO₃
Color White to off-white
SMILES

O=C(O)CCC1=CC=C(NCC2=CC=CC(OC3=CC=CC=C3)=C2)C=C1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

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.
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.
Am J Respir Cell Mol Biol

An Antiviral Effect of Linoleic Acid Against Rhinovirus Infection. [Abstract]

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).
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

Lösungsmittel & Löslichkeit

In Vitro:

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.8784 mL

14.3922 mL

28.7844 mL

5 mM

0.5757 mL

2.8784 mL

5.7569 mL

10 mM

0.2878 mL

1.4392 mL

2.8784 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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 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.

Protocol 2

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.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (7.20 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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

8 Cited Publications

100 mg Angebot einholen

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GW9508

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

Membrane Transporter/Ion Channel Compound Library

Anti-diabetic Compound Library

Anti-Cardiovascular Disease Compound Library

Neuroprotective Compound Library

Lipid Metabolism Compound Library

Targeted Diversity Library

Potassium Channel Compound Library

Human Metabolite Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Activators Library

Ion Channel Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) GW9508

Alle Free Fatty Acid Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (8)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GW9508

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

Membrane Transporter/Ion Channel Compound Library

Anti-diabetic Compound Library

Anti-Cardiovascular Disease Compound Library

Neuroprotective Compound Library

Lipid Metabolism Compound Library

Targeted Diversity Library

Potassium Channel Compound Library

Human Metabolite Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Activators Library

Ion Channel Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) GW9508

Alle Free Fatty Acid Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (8)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GW9508 Related Classifications

HY-15589 Related Classifications