GLPG0974

Name: GLPG0974
Brand: MedChemExpress
SKU: HY-12940
Rating: 5.0 (17 reviews)

Cat. No.: HY-12940 Purity: 98.12% ee.: 98.57%: Data Sheet
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GLPG0974 is a free fatty acid receptor-2 (FFA2/GPR43) antagonist with an IC₅₀ of 9 nM.

For research use only. We do not sell to patients.

CAS No. : 1391076-61-1

Size	Stock	Quantity

Free Sample (0.1 - 0.2 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 17 publication(s) in Google Scholar

Other Forms of GLPG0974:

(S)-GLPG0974 In-stock

17 Publications Citing Use of MCE GLPG0974

In Vivo Efficacy Study

RT-PCR

Histological Imaging/Staining

IHC

Flow Cytometry

: 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.

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

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

IC₅₀ & Target

IC50: 9 nM (GPR43)^[1]

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

Molecular Weight

485.00

Formula

C₂₅H₂₅ClN₂O₄S

CAS No.

1391076-61-1

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 98.12% ee.: 98.57%

Select Batch:

Data Sheet (276 KB) SDS (252 KB)

COA (252 KB) HNMR (140 KB) NP-HPLC (337 KB) LCMS (121 KB)

Handling Instructions (2659 KB)

References

[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]

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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[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]

Complete Stock Solution Preparation Table

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

GLPG0974 Related Classifications

Metabolic Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GLPG09741391076-61-1GLPG 0974GLPG-0974Free Fatty Acid ReceptorFFARInhibitorinhibitorinhibit

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GLPG0974

Customer Review

Other Forms of GLPG0974:

GLPG0974 Related Antibodies

17 Publications Citing Use of MCE GLPG0974

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Free Fatty Acid Receptor Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

GLPG0974 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

GLPG0974 Related Classifications

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