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GLPG0974 

Cat. No.: HY-12940
Handling Instructions

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.

GLPG0974 Chemical Structure

GLPG0974 Chemical Structure

CAS No. : 1391076-61-1

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

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]

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].

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].

Clinical Trial
Solvent & Solubility
In Vitro: 

10 mM in 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
*Please refer to the solubility information to select the appropriate solvent.
References
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
Molecular Weight

485.00

Formula

C₂₅H₂₅ClN₂O₄S

CAS No.

1391076-61-1

SMILES

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

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
GLPG0974
Cat. No.:
HY-12940
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GLPG0974

Cat. No.: HY-12940