Art. -Nr.: HY-12940

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GLPG0974

18 Cited Publications

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Based on 18 publication(s) in Google Scholar

GLPG0974 is a free fatty acid receptor-2 (FFA2/GPR43) antagonist with an IC₅₀ of 9 nM.

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Reinheit: 98.12%
CAS. Nr.: 1391076-61-1
Formel: C₂₅H₂₅ClN₂O₄S
Molecular Weight:485.00

Speicherung:

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

GLPG0974 Chemical Structure

CAS. Nr.: 1391076-61-1

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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
- Clinical Trial
Chemical Information
Publications (18)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

GLPG0974 is a free fatty acid receptor-2 (FFA2/GPR43) antagonist with an IC₅₀ of 9 nM.

IC₅₀ & Target

IC50: 9 nM (GPR43)^[1]

Alle Free Fatty Acid Receptor Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	9 nM Compound: 99, GLPG0974	Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization	[PMID: 25380412]
Neutrophil	IC₅₀	27 nM Compound: 99, GLPG0974	Inhibition of sodium acetate-induced cell migration of human neutrophils after 1 hr by ATP luminescence based assay Inhibition of sodium acetate-induced cell migration of human neutrophils after 1 hr by ATP luminescence based assay	[PMID: 25380412]
Neutrophil	IC₅₀	43 nM Compound: 99, GLPG0974	Inhibition of sodium acetate-induced cell migration of human neutrophils after 1 hr in presence of 90% plasma by ATP luminescence based assay Inhibition of sodium acetate-induced cell migration of human neutrophils after 1 hr in presence of 90% plasma by ATP luminescence based assay	[PMID: 25380412]

In Vitro

GLPG0974 is able to inhibit acetate-induced neutrophil migration strongly in vitro and demonstrates ability to inhibit a neutrophil-based pharmacodynamic (PD) marker, CD11b activation-specific epitope [AE], in a human whole blood assay^[1].

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

In Vivo

GLPG0974 shows excellent pharmacokinetic properties in rat with a bioavailability of 47% and a linear increase of the plasma exposure after oral dosing at 5 and 30 mg/kg. The extended half-life observed following the increase of oral dose is consistent with the project objective to obtain long target coverage in human^[1].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1391076-61-1
Appearance Solid
Molecular Weight 485.00
Formel C₂₅H₂₅ClN₂O₄S
Color Off-white to light yellow
SMILES

O=C(O)CCCN(C([C@]1(C)N(C(C2=CSC3=CC=CC=C32)=O)CC1)=O)CC4=CC=CC(Cl)=C4
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 (18)

All In Vivo Efficacy StudyRT-PCRHistological Imaging/StainingIHCFlow Cytometry

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Journal Impact Factor

Cancer Cell

Fusobacterium nucleatum facilitates anti-PD-1 therapy in microsatellite stable colorectal cancer. [Abstract]

2024 Oct 14;42(10):1729-1746.e8. PMID: 39303724
Cell Host Microbe

Oat-β-glucan potentiates anti-PD-1 efficacy through Faecalibacterium prausnitzii-derived butyrate and indole-3-propionic acid. [Abstract]

2026 Jul 8;34(7):1333-1349.e10. PMID: 42214334
Cell Host Microbe

Roseburia intestinalis-derived butyrate alleviates neuropathic pain. [Abstract]

2025 Jan 8;33(1):104-118.e7. PMID: 39706182
Nat Commun

Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]

2026 Feb 12;17(1):1214. PMID: 41680175
J Adv Res

Strain specificity of lactobacilli with promoted colonization by galactooligosaccharides administration in protecting intestinal barriers during Salmonella infection. [Abstract]

2024 Feb:56:1-14. PMID: 36894120
Redox Biol

EGCG drives gut microbial remodeling-induced epithelial GPR43 activation to lessen Th1 polarization in colitis. [Abstract]

2024 Sep:75:103291. PMID: 39116526
Adv Sci (Weinh)

The Probiotic Parabacteroides johnsonii Ameliorates Metabolic Disorders Through Promoting BCAAs to BSCFAs Conversion. [Abstract]

2025 Aug 7:e02624. PMID: 40772426
Phytomedicine

Tetrastigma hemsleyanum polysaccharides alleviate inflammatory bowel disease via the gut microbiota-SCFA-GPR43 signaling axis. [Abstract]

2025 Dec:149:157523. PMID: 41308392

GLPG0974 purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2025 Dec:149:157523. [Abstract]

THP (Tetrastigma hemsleyanum polysaccharides, THP) or 4-CMTB (10 mg/kg, i.p., 5 days) improved the Disease Activity Index induced by DSS. However, GLPG0974 (1 mg/kg, i.g., 5 days) reversed the Disease Activity Index increase induced by Tetrastigma hemsleyanum polysaccharides in the IBD mouse model.

GLPG0974 purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2025 Dec:149:157523. [Abstract]

THP(Tetrastigma hemsleyanum polysaccharides, THP) or 4-CMTB (10 mg/kg, i.p., 5 days) reduced the expression of these pro-inflammatory mediators (IL-6, IL-1β, TNFα, and MCP-1) in the colon. Conversely, mice administered THP + GLPG0974 (1 mg/kg, i.g., 5 days) displayed an upregulation of colonic cytokine mRNA.

GLPG0974 purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2025 Dec:149:157523. [Abstract]

THP (Tetrastigma hemsleyanum polysaccharides, THP)or 4-CMTB (10 mg/kg, i.p., 5 days) reduced the abnormal spleen index induced by DSS and improved the pathological changes in the spleens of mice following DSS treatment. Conversely, in the THP + GLPG0974 group, the abnormal spleen index and spleen inflammation persisted, indicating that GLPG0974 reversed the therapeutic effect of THP.

GLPG0974 purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2025 Dec:149:157523. [Abstract]

Immunohistochemical staining images of Ki67 showed that THP (Tetrastigma hemsleyanum polysaccharides, THP) or 4-CMTB (10 mg/kg, i.p., 5 days) regulated the growth and apoptosis of intestinal epithelial cells induced by DSS in mice. However, mice in the THP + GLPG0974 group exhibited persistent damage to intestinal epithelial cells.

GLPG0974 purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2025 Dec:149:157523. [Abstract]

THP (Tetrastigma hemsleyanum polysaccharides, THP) or 4-CMTB alleviated the aberrant proliferation of CD3+ cells induced by DSS in mice. However, mice in the THP + GLPG0974 group still exhibited elevated levels of CD3+ cells.
Journal of Future Foods

2026 Jan 2.
J Anim Sci Biotechnol

Regulation of serotonin production by specific microbes from piglet gut. [Abstract]

2023 Aug 5;14(1):111. PMID: 37542282
Chin Med

Shaoyao Decoction reduced T lymphocyte activation by regulating of intestinal flora and 5-hydroxytryptamine metabolism in ulcerative colitis. [Abstract]

2024 Jun 15;19(1):87. PMID: 38879471
Biochem Pharmacol

MNAM enhances Blautia abundance and modulates Th17/Treg balance to alleviate diabetes in T2DM mice. [Abstract]

2024 Dec;230(Pt 2):116593. PMID: 39454734
Int J Mol Sci

Gut Microbiota-Derived Propionic Acid Mediates ApoA-I-Induced Amelioration of MASLD via Activation of GPR43-Ca2+-CAMKII-ATGL Hepatic Lipolysis. [Abstract]

2026 Jan 1;27(1):468. PMID: 41516340
Immunology

Dietary human milk oligosaccharides reduce allergic airway inflammation by modulating SCFAs level and ILC2 activity. [Abstract]

2024 Nov;173(3):562-574. PMID: 39108003
Biology (Basel)

Exercise Ameliorates Insulin Resistance of Type 2 Diabetes through Motivating Short-Chain Fatty Acid-Mediated Skeletal Muscle Cell Autophagy. [Abstract]

2020 Aug 3;9(8):203. PMID: 32756447
J Appl Microbiol

Houpo Paiqi Mixture Promotes Intestinal Motility in Constipated Rats by Modulating Gut Microbiota and Activating 5-HT-cAMP-PKA Signal Pathway. [Abstract]

2023 Aug 1;134(8):lxad153. PMID: 37481692
SSRN

2026 Mar 2.
bioRxiv

2023 Dec 10.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 200 mg/mL (412.37 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

2.0619 mL

10.3093 mL

20.6186 mL

5 mM

0.4124 mL

2.0619 mL

4.1237 mL

10 mM

0.2062 mL

1.0309 mL

2.0619 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: 5 mg/mL (10.31 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: 5 mg/mL (10.31 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (10.31 mM); Clear solution

This protocol yields a clear solution of ≥ 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 (50.0 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

Protokoll

Animal Administration^[1]

Rats^[1]

GLPG0974 is orally dosed as a single esophageal gavage at 5−10 mg/kg and intravenously dosed as a bolus via the caudal vein at 1 mg/kg to male Sprague−Dawley rats. Each group consisted of three rats. Blood samples are collected^[1].

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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]. Pizzonero M, et al. Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic. J Med Chem. 2014 Dec 11;57(23):10044-57. [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	2.0619 mL	10.3093 mL	20.6186 mL	51.5464 mL
	5 mM	0.4124 mL	2.0619 mL	4.1237 mL	10.3093 mL
	10 mM	0.2062 mL	1.0309 mL	2.0619 mL	5.1546 mL
	15 mM	0.1375 mL	0.6873 mL	1.3746 mL	3.4364 mL
	20 mM	0.1031 mL	0.5155 mL	1.0309 mL	2.5773 mL
	25 mM	0.0825 mL	0.4124 mL	0.8247 mL	2.0619 mL
	30 mM	0.0687 mL	0.3436 mL	0.6873 mL	1.7182 mL
	40 mM	0.0515 mL	0.2577 mL	0.5155 mL	1.2887 mL
	50 mM	0.0412 mL	0.2062 mL	0.4124 mL	1.0309 mL
	60 mM	0.0344 mL	0.1718 mL	0.3436 mL	0.8591 mL
	80 mM	0.0258 mL	0.1289 mL	0.2577 mL	0.6443 mL
	100 mM	0.0206 mL	0.1031 mL	0.2062 mL	0.5155 mL

Keywords

GLPG0974

18 Cited Publications

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GLPG0974

Chemical Probe Library

Targeted Diversity Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Publications Citing Use of MedChemExpress (MCE) GLPG0974

Alle Free Fatty Acid Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (18)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GLPG0974

Chemical Probe Library

Targeted Diversity Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Publications Citing Use of MedChemExpress (MCE) GLPG0974

Alle Free Fatty Acid Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (18)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GLPG0974 Related Classifications

HY-12940 Related Classifications