1391076-61-1
1391076-61-1 structure
- Name: GLPG 0974
- Chemical Name: GLPG0974
- CAS Number: 1391076-61-1
- Molecular Formula: C25H25ClN2O4S
- Molecular Weight: 485.00
- Catalog: Research Areas Metabolic Disease
- Create Date: 2019-02-08 20:34:22
- Modify Date: 2024-01-06 00:27:39
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GLPG0974 is a free fatty acid receptor-2 (FFA2/GPR43) antagonist with an IC50 of 9 nM.
| Name | GLPG0974 |
|---|
| Description | GLPG0974 is a free fatty acid receptor-2 (FFA2/GPR43) antagonist with an IC50 of 9 nM. |
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| Related Catalog | |
| 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]. |
| Animal Admin | 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]. |
| References |
| Molecular Formula | C25H25ClN2O4S |
|---|---|
| Molecular Weight | 485.00 |