SML2443

GLPG0974

≥98% (HPLC)

• Synonym(s): 4-[[(R)-1-(Benzo[b]thiophene-3-carbonyl)-2-methyl-azetidine-2-carbonyl]-(3-chloro-benzyl)-amino]-butyric acid, GLPG 0974, GLPG-0974
• Empirical Formula (Hill Notation): C₂₅H₂₅ClN₂O₄S
• CAS Number: 1391076-61-1
• Molecular Weight: 485.00
• MDL番号: MFCD28502087

Properties

• アッセイ: ≥98% (HPLC)
• 形状: powder
• 光学活性: [α]/D +175 to +200°, c = 1 in chloroform-d
• 色: white to beige
• 溶解性: DMSO: 2 mg/mL, clear
• 保管温度: 2-8°C
• SMILES string: O=C(C1=CSC2=C1C=CC=C2)N3CC[C@]3(C)C(N(CC4=CC=CC(Cl)=C4)CCCC(O)=O)=O

Description

生物化学的／生理学的作用

GLPG0974 is an orally available, high-affinity, potent 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.).

Safety Information

• 保管分類コード: 13 - Non Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable