Referencia número: HY-50691

GW-1100

Name: GW-1100
Brand: MedChemExpress
SKU: HY-50691
Price: 71.00 USD
Availability: InStock
Rating: 5 (22 reviews)

22 Cited Publications

Revisión del cliente

Based on 22 publication(s) in Google Scholar

GW-1100 is a selective GPR40 antagonist with a pIC₅₀ of 6.9.

Para uso exclusivo en investigación. No vendemos a pacientes.

Pureza : 97.16%
No. CAS: 306974-70-9
Fòrmula: C₂₇H₂₅FN₄O₄S
Peso molecular:520.58

Almacenamiento:

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

GW-1100 Chemical Structure

No. CAS: 306974-70-9

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (22)
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

GW-1100 is a selective GPR40 antagonist with a pIC₅₀ of 6.9.

IC₅₀ & Target

pIC50: 6.9 (GPR40)^[1]

Ver todos los productos específicos de isoformas Free Fatty Acid Receptor :

In Vitro

GW-1100 (GW1100) dose dependently inhibits GPR40-mediated Ca²⁺ elevations stimulated by GW9508 and linoleic acid (pIC₅₀ values of 5.99±0.03 and 5.99±0.06, respectively). GW-1100 at a concentration of 1 μM produces a significant rightward shift in the concentration-response curve to GW9508 (pEC₅₀=7.17±0.08 in the absence and pEC₅₀=6.79±0.09 in the presence of 1 μM GW-1100; P<0.05; n=3). At concentrations of GW-1100 of 3 μM and higher a significant decrease in the maximal response is observed with a continuing rightward shift in the pEC₅₀ response^[2]. GW-1100 (GW1100) reduces FFAR1 ligand-induced intracellular calcium in CHO-K1/bFFAR1 cells and neutrophils. CHO-K1/bFFAR1 cells are incubated for 15 min with 10 μM GW1100 or vehicle (0.1% DMSO) and then stimulated with vehicle, oleic acid, linoleic acid or GW9508. GW-1100 significantly reduces the increase in intracellular calcium induced by 300 μM oleic acid (AUC_{(60-150 s)}, p<0.05), 100 μM linoleic acid (AUC_{(60-150 s)}, p<0.05) and 10 μM GW9508 (AUC_{(60-150 s)}, p<0.05)^[3].

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

In Vivo

The intracerebroventricular injection of DHA (50 μg) and GW9508 (1.0 μg), a GPR40-selective agonist, significantly reduces mechanical allodynia and thermal hyperalgesia at day 7, but not at day 1, after CFA injection. These effects are inhibited by intracerebroventricular pretreatment with GW-1100 (10 μg), a GPR40 antagonist^[4].

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

Chemical Information

No. CAS 306974-70-9
Appearance Solid
Peso molecular 520.58
Fòrmula C₂₇H₂₅FN₄O₄S
Color White to off-white
SMILES

O=C1C(CC2=CN=C(N=C2)OCC)=CN(C(SCC3=CC=C(C=C3)F)=N1)C4=CC=C(C(OCC)=O)C=C4
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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

Publications (22)

All Bio/Physico-chemical AssayCell Imaging/StainingIFWB

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Journal Impact Factor

Cell Metab

Microbial-derived 3-phenylpropionic acid orchestrates immune-progenitor cell crosstalk to promote beige adipogenesis and energy expenditure. [Abstract]

2026 Apr 7;38(4):763-778.e7. PMID: 41742426
Aging Cell

2026 Jul;25(7):e70630. PMID: 42444033
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
J Agric Food Chem

Activating Effects of Phenolics from Apache Red Zea mays L. on Free Fatty Acid Receptor 1 and Glucokinase Evaluated with a Dual Culture System with Epithelial, Pancreatic, and Liver Cells. [Abstract]

2019 Aug 21;67(33):9148-9159. PMID: 30785272

GW-1100 purchased from MedChemExpress. Usage Cited in: J Agric Food Chem. 2019 Aug 21;67(33):9148-9159. [Abstract]

Effect of phenolic-rich extracts from red maize in GSIS in iNS-1E pancreatic β cells. The cells were treated with different concentrations RPE (0.125–1 mg/mL) and a FFAR1 agonist TAK-875 (5–20 μM). Additionally, the highest concentration of each treatment was tested in the presence or absence of 10 μM GW-1100.

GW-1100 purchased from MedChemExpress. Usage Cited in: J Agric Food Chem. 2019 Aug 21;67(33):9148-9159. [Abstract]

Effect of RPE on insulin secretion on glucose-starved INS-1E pancreatic cells. The cells were treated with 1 mg/mL RPE or 20 μM TAK-875 in the presence or absence of 10 μM GW-1100.
Biochem Pharmacol

GPR40 inhibits microglia-mediated neuroinflammation via the NLRP3/IL-1β/glutaminase pathway after subarachnoid hemorrhage. [Abstract]

2025 Aug:238:116971. PMID: 40318813

GW-1100 purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2025 Aug:238:116971. [Abstract]

GW1100 at 10 μM for 15 min. Dihydroergotamine (DHE) staining of the ctr, GW9508, GW9508 + GW1100, Hb, Hb + GW9508 and Hb + GW9508 + GW1100 groups. Scale bar = 20 μm. Arrow indicated superoxide anion production.

GW-1100 purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2025 Aug:238:116971. [Abstract]

GW1100 at 10 μM for 15 min. Relative ROS levels in the neurons of the the ctr, GW9508, GW9508 + GW1100, Hb, Hb + GW9508 and Hb + GW9508 + GW1100 groups.

GW-1100 purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2025 Aug:238:116971. [Abstract]

GW1100 at 10 μM for 15 min. Fluoro-Jade C (FJC) staining of the ctr, GW9508, GW9508 + GW1100, Hb, Hb + GW9508 and Hb + GW9508 + GW1100 groups.

GW-1100 purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2025 Aug:238:116971. [Abstract]

GW1100 at 10 μM for 15 min. Immunofluorescence staining for NLRP3 (red), Iba-1 (green) and GPR40 (violet) in the ctr, GW9508, GW9508 + GW1100, Hb, Hb + GW9508 and Hb + GW9508 + GW1100 groups. I Quantification of microglial NLRP3 immunofluorescent intensity in the ctr, GW9508, GW9508 + GW1100, Hb, Hb + GW9508 and Hb + GW9508 + GW1100 groups.

GW-1100 purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2025 Aug:238:116971. [Abstract]

GW1100 at 10 μM for 15 min. Representative western blot images of glutaminase expression in ctr, GW9508, GW9508 + GW1100, SAH, SAH + GW9508, SAH + GW9508 + GW1100 groups.

GW-1100 purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2025 Aug:238:116971. [Abstract]

GW1100 (5 mg/kg) was administrated intraperitoneally at 1 h after SAH. Representative western blotting of GPR40, cAMP, p-PKA, PKA, ASC, NLRP3, cleaved caspase-1, and cleaved IL-1β expression in ctr, GW9508, GW9508 + GW1100, SAH, SAH + GW9508, and SAH + GW9508 + GW1100 groups.

GW-1100 purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2025 Aug:238:116971. [Abstract]

GW1100 (5 mg/kg) was administrated intraperitoneally at 1 h after SAH. Fluoro-Jade C (FJC) staining of the ctr, GW9508, GW9508 + GW1100, SAH, SAH + GW9508, and SAH + GW9508 + GW1100 groups. Scale bar = 50 μm.
RSC Adv

Label-free cell phenotypic study of FFA4 and FFA1 and discovery of novel agonists of FFA4 from natural products. [Abstract]

2019 May 15;9(26):15073-15083. PMID: 35516320
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
J Endocrinol

Vincamine as a GPR40 agonist improves glucose homeostasis in type 2 diabetic mice. [Abstract]

2019 Feb 1;240(2):195-214. PMID: 30400036

GW-1100 purchased from MedChemExpress. Usage Cited in: J Endocrinol. 2019 Feb 1;240(2):195-214. [Abstract]

Western analysis of p-Akt, t-Akt and IRS2 in the treatment of STZ, GW1100 or Vin.
Molecules

Ginseng Gintonin Contains Ligands for GPR40 and GPR55. [Abstract]

2020 Mar 2;25(5):1102. PMID: 32121640
Sci Rep

The dual DPP4 inhibitor and GPR119 agonist HBK001 regulates glycemic control and beta cell function ex and in vivo. [Abstract]

2017 Jun 28;7(1):4351. PMID: 28659588
Am J Pathol

Tumor necrosis factor α decreases glucagon-like peptide-2 expression by up-regulating G-protein-coupled receptor 120 in Crohn disease. [Abstract]

2015 Jan;185(1):185-96. PMID: 25447053
Neuropharmacology

GW9508 ameliorates cognitive impairment via the cAMP-CREB and JNK pathways in APPswe/PS1dE9 mouse model of Alzheimer's disease. [Abstract]

2020 Mar 1:164:107899. PMID: 31809762
BMC Cancer

Palmitic acid-activated GPRs/KLF7/CCL2 pathway is involved in the crosstalk between bone marrow adipocytes and prostate cancer. [Abstract]

2024 Jan 15;24(1):75. PMID: 38221626
Naunyn Schmiedebergs Arch Pharmacol

Effect of omega-3 fatty acids on glucose homeostasis: role of free fatty acid receptor 1. [Abstract]

2020 Oct;393(10):1797-1808. PMID: 32388601
Nutr Metab

PA and OA induce abnormal glucose metabolism by inhibiting KLF15 in adipocytes. [Abstract]

2021 Nov 21;18(1):100. PMID: 34802421
J Diabetes Res

Pioglitazone Ameliorates Atorvastatin-Induced Islet Cell Dysfunction through Activation of FFA1 in INS-1 Cells. [Abstract]

2019 Feb 3:2019:5245063. PMID: 30863781
Mol Cell Endocrinol

Fatty acids as a direct regulator of aldosterone hypersecretion. [Abstract]

2023 Feb 5:561:111836. PMID: 36549461
Psychopharmacology

GPR40 receptor agonist TAK-875 improves cognitive deficits and reduces β-amyloid production in APPswe/PS1dE9 mice. [Abstract]

2021 Aug;238(8):2133-2146. PMID: 34173034
Animals (Basel)

Divergent Regulation of Mammary Lipogenesis by trans-10, cis-12 and cis-9, trans-11 CLA Isomers Is Determined by Receptor-Specific Signaling. [Abstract]

2025 Nov 26;15(23):3418. PMID: 41375476
PLoS One

Anthocyanins from purple corn activate free fatty acid-receptor 1 and glucokinase enhancing in vitro insulin secretion and hepatic glucose uptake. [Abstract]

2018 Jul 11;13(7):e0200449. PMID: 29995924
Braz J Pharm Sci

2023, 58.
Research Square Preprint

2023 Aug 14.

Solvente y solubilidad

In Vitro:

DMSO : 50 mg/mL (96.05 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

1.9209 mL

9.6047 mL

19.2093 mL

5 mM

0.3842 mL

1.9209 mL

3.8419 mL

10 mM

0.1921 mL

0.9605 mL

1.9209 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.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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 50% PBS

Solubility: 5 mg/mL (9.60 mM); Suspended solution; Need ultrasonic

Protocol 2

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

Solubility: ≥ 2.5 mg/mL (4.80 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.

Protocol 3

Add each solvent one by one: 1% DMSO 99% Saline

Solubility: 0.06 mg/mL (0.12 mM); Suspended solution; Need ultrasonic

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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (280 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Stoddart LA, et al. Uncovering the pharmacology of the G protein-coupled receptor GPR40: high apparent constitutive activity in guanosine 5'-O-(3-[35S]thio)triphosphate binding studies reflects binding of an endogenous agonist. Mol Pharmacol. 2007 Apr;71( [Content Brief]

[2]. 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]

[3]. Manosalva C, et al. Cloning, identification and functional characterization of bovine free fatty acid receptor-1 (FFAR1/GPR40) in neutrophils. PLoS One. 2015 Mar 19;10(3):e0119715. [Content Brief]

[4]. Nakamoto K, et al. Hypothalamic GPR40 signaling activated by free long chain fatty acids suppresses CFA-induced inflammatorychronic pain. PLoS One. 2013 Dec 12;8(12):e81563. [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	1.9209 mL	9.6047 mL	19.2093 mL	48.0234 mL
	5 mM	0.3842 mL	1.9209 mL	3.8419 mL	9.6047 mL
	10 mM	0.1921 mL	0.9605 mL	1.9209 mL	4.8023 mL
	15 mM	0.1281 mL	0.6403 mL	1.2806 mL	3.2016 mL
	20 mM	0.0960 mL	0.4802 mL	0.9605 mL	2.4012 mL
	25 mM	0.0768 mL	0.3842 mL	0.7684 mL	1.9209 mL
	30 mM	0.0640 mL	0.3202 mL	0.6403 mL	1.6008 mL
	40 mM	0.0480 mL	0.2401 mL	0.4802 mL	1.2006 mL
	50 mM	0.0384 mL	0.1921 mL	0.3842 mL	0.9605 mL
	60 mM	0.0320 mL	0.1601 mL	0.3202 mL	0.8004 mL
	80 mM	0.0240 mL	0.1201 mL	0.2401 mL	0.6003 mL

Bioz

Keywords

GW-1100

22 Cited Publications

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GW-1100

Publications Citing Use of MedChemExpress (MCE) GW-1100

Ver todos los productos específicos de isoformas Free Fatty Acid Receptor