GW-1100
Based on 21 publication(s) in Google Scholar
GW-1100 is a selective GPR40 antagonist with a pIC50 of 6.9.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 97.16%
- CAS No.: 306974-70-9
- Formule: C27H25FN4O4S
- Masse moléculaire:520.58
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Publications Citing Use of MedChemExpress (MCE) GW-1100
More- Cell Metab. 2026 Apr 7;38(4):763-778.e7. [Abstract]
- Cell Rep. 2024 Oct 10;43(10):114858. [Abstract]
- J Agric Food Chem. 2019 Aug 21;67(33):9148-9159. [Abstract]
- Biochem Pharmacol. 2025 May 1:116971. [Abstract]
- RSC Adv. 2019 May 15;9(26):15073-15083. [Abstract]
- Eur J Pharmacol. 2021 Oct 15:909:174362. [Abstract]
- J Endocrinol. 2019 Feb 1;240(2):195-214. [Abstract]
- Molecules. 2020 Mar 2;25(5):1102. [Abstract]
- Sci Rep. 2017 Jun 28;7(1):4351. [Abstract]
- Am J Pathol. 2015 Jan;185(1):185-96. [Abstract]
- Neuropharmacology. 2020 Mar 1;164:107899. [Abstract]
- BMC Cancer. 2024 Jan 15;24(1):75. [Abstract]
- Naunyn Schmiedebergs Arch Pharmacol. 2020 Oct;393(10):1797-1808. [Abstract]
- Nutr Metab. 2021 Nov 21;18(1):100. [Abstract]
- J Diabetes Res. 2019 Feb 3:2019:5245063. [Abstract]
- Mol Cell Endocrinol. 2023 Feb 5:561:111836. [Abstract]
- Psychopharmacology. 2021 Aug;238(8):2133-2146. [Abstract]
- Animals (Basel). 2025 Nov 26;15(23):3418. [Abstract]
- PLoS One. 2018 Jul 11;13(7):e0200449. [Abstract]
- Braz J Pharm Sci. 2023, 58.
- Research Square Preprint. 2023 Aug 14.
Customer Validation & Images
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Cell Imaging/Staining
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Bio/Physico-chemical Assay
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Cell Imaging/Staining
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IF
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WB
Activité biologique
pIC50: 6.9 (GPR40)[1]
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 306974-70-9
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Appearance Solid
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Masse moléculaire 520.58
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Formule C27H25FN4O4S
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Color White to off-white
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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
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (21)
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Journal Impact Factor
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Most Recent
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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 -
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.
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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
GW-1100 purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2025 May 1:116971. [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 May 1:116971. [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 May 1:116971. [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 May 1:116971. [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 May 1:116971. [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 May 1:116971. [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 May 1:116971. [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.
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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
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.
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Molecules
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
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
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 -
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Solvant et solubilité
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)
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: 1% DMSO 99% Saline
Solubility: 0.06 mg/mL (0.12 mM); Suspended solution; Need ultrasonic
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.
Protocole
CHO-K1/bFFAR1 or CHO-K1/pcDNA3.1 cells (2×106 cells/2 mL) are loaded with 2.5 μM Fura-2AM fluorescent indicator dye in recording buffer (10 mM HEPES, 140 mM NaCl, 2 mM CaCl2, 21 mM MgCl2, 25 mM KCl, 10 mM glucose, pH 7.4) for 30 min, washed three times with recording buffer, and returned to the incubator for 10 min. Cells are incubated with different concentrations of propionic acid (1, 10 and 30 mM), oleic acid (0-500 μM), linoleic acid (0-200 μM), GW9508 (0-100 μM), ionomycin (2 μM), thapsigargin (2 μM) or vehicle (0.1% DMSO). The fatty acid concentrations used in all experiments are in the range of concentrations of healthy and peripartum cows. In another set of experiments, cells are incubated with either 10 μM GW-1100 for 15 min, 2 μM U73122 for 3 min or vehicle (0.1% DMSO) for 15 min and then stimulated with either 300 μM oleic acid, 100 μM linoleic acid or 10 μM GW9508. Cellular fluorescence (Ca2+) is measured at 509 nm emission with 340/380 nm dual wavelength excitation using a LS55 spectrofluorimeter. Cuvette temperatures are maintained at 37°C with constant stirring[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[4]
Male ddY mice (age, 4 weeks) are housed in cages at 23-24°C with a 12-h light-dark cycle (lights from 8 am to 8 pm) and food and waterad libitum. DHA (50 µg/mouse), the selective GPR40-agonist GW9508 (1.0-25 µg/mouse) and the GPR40 antagonist GW1100 (1-10 µg/mouse) are dissolved in 1% DMSO and the solution is diluted with saline before von Frey testing (1% DMSO final concentration). The doses of GW9508 are chosen based upon our previous publication, whereas GW-1100 is selected on the basis of previous reports and our preliminary experiments. Under a non-anesthetized state, DHA and GW9508 are administered via the intracerebroventricular (i.c.v.) route 10 min before CFA injection, and GW1100 is administered via the i.c.v. route 10 min before GW9508 injection. Flavopiridol (5 and 15 nmol/mouse), a cyclin-dependent kinase inhibitor, is administered by i.c.v. injection into the left lateral ventricle of the mice twice a day (at 9:00 and 19:00) after CFA treatment.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (280 KB)
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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)
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Instruction de manipulation (2659 KB)
Références
[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]
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 | 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 |
GW-1100 Related Classifications
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