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GLPG0974

品牌
Sigma-Aldrich
CAS
1391076-61-1
货号
SML2443
规格纯度
≥98% (HPLC)
价格
1536.83 *本价格含增值税费
促销
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数量
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半岛bd体育手机客户端 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
半岛bd体育手机客户端 介绍:

半岛bd体育手机客户端 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 exhibitsin vivoefficacy (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

半岛bd体育手机客户端 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

Sigma-Aldrich

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