| Identification | Back Directory | [Name]
MPMKMQHJHDHPBE-RUZDIDTESA-N | [CAS]
1391076-61-1 | [Synonyms]
GLPG 0974
(GLPG0974)
MPMKMQHJHDHPBE-RUZDIDTESA-N
4-[[[(2R)-1-(Benzo[b]thien-3-ylcarbonyl)-2-methyl-2-azetidinyl]carbonyl][(3-chlorophenyl)methyl]amino]butanoic acid
Butanoic acid, 4-[[[(2R)-1-(benzo[b]thien-3-ylcarbonyl)-2-methyl-2-azetidinyl]carbonyl][(3-chlorophenyl)methyl]amino]- | [Molecular Formula]
C25H25ClN2O4S | [MDL Number]
MFCD28502087 | [MOL File]
1391076-61-1.mol | [Molecular Weight]
484.99 |
| Chemical Properties | Back Directory | [Boiling point ]
726.3±60.0 °C(Predicted) | [density ]
1.374±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: soluble; Ethanol: soluble | [form ]
A solid | [pka]
4.63±0.10(Predicted) | [color ]
Off-white to light yellow | [Optical Rotation]
[α]/D +175 to +200°, c =1 in chloroform-d | [InChIKey]
MPMKMQHJHDHPBE-RUZDIDTESA-N | [SMILES]
O=C(C1=CSC2=C1C=CC=C2)N3CC[C@]3(C)C(N(CC4=CC=CC(Cl)=C4)CCCC(O)=O)=O |
| Hazard Information | Back Directory | [Uses]
GLPG 0974 is a potent FFA2 antagonist. | [Biological Activity]
GLPG0974 is an orally availablehigh-affinitypotent and selective free fatty acid receptor 2 (FFA2; FFAR2; GPCR43; GPR43) antagonist (hFFA2 Kd = 7.5 nM; IC50 = 9 nM; Na acetate EC80-induced Ca2+ flux in HEK293 hFFA2 transfectants) with little potency toward 55 other receptors/channels/transporters (IC50 >10 μM)including FFA3 (GPR41). GLPG0974 inhibits acetate-induced human neutrophil migration (IC50 = 27 nM) and exhibits in vivo efficacy (0.1 or 1 mg/kg intragastrically) against duodenal lesions induction by NSAID indomethacin/FFA2 agonist phenylacetamide-1 co-treatment with good pharmacokinetic properties and oral availability (F = 47% in rats; 5 mg/kg p.o.). | [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]. | [storage]
Store at +4°C |
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| Company Name: |
cjbscvictory
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| Tel: |
13348960310 13348960310 |
| Website: |
www.weikeqi-biotech.com/ |
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