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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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50 mg USD 980 Ask For Quote & Lead Time
100 mg USD 1800 Ask For Quote & Lead Time

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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
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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility
In Vitro: 

DMSO : 200 mg/mL (412.37 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

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.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 5 mg/mL (10.31 mM); Clear solution

*All of the co-solvents are provided by MCE.
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
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Keywords:

GLPG0974GLPG 0974GLPG-0974OthersInhibitorinhibitorinhibit

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GLPG0974
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HY-12940
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