GLPG0974

产品名称：

1391076-61-1
GLPG0974
GLPG 0974
GLPG-0974
4-[[(R)-1-(Benzo[b]thiophene-3-carbonyl)-2-methyl-azetidine-2-carbonyl]-(3-chloro-benzyl)-amino]-butyric acid

产品介绍：

产品说明

生化/生理作用

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.).

基本信息

经验(实验)分子式	C₂₅H₂₅ClN₂O₄S
分子量	485.00
MDL编号	MFCD28502087

产品性质

测定	≥98% (HPLC)
形式	powder
旋光性	[α]/D +175 to +200°, c = 1 in chloroform-d
颜色	white to beige
溶解性	DMSO: 2 mg/mL, clear
储存温度	2-8℃
SMILES string	O=C(C1=CSC2=C1C=CC=C2)N3CC[C@]3(C)C(N(CC4=CC=CC(Cl)=C4)CCCC(O)=O)=O

安全信息

储存分类代码	13 - Non Combustible Solids
WGK	WGK 3
闪点(F)	Not applicable
闪点(C)	Not applicable