检测方案
≥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°C
SMILES字符串
O=C(C1=CSC2=C1C=CC=C2)N3CC[C@]3(C)C(N(CC4=CC=CC(Cl)=C4)CCCC(O)=O)=O
生化/生理作用
GLPG0974是一种口服，高亲和力，有效和选择性的游离脂肪酸受体2（FFA2；FFAR2；GPCR43；GPR43）拮抗剂（hFFA2 Kd=7.5 nM；IC50=9 nM；乙酸钠EC80诱导的HEK293 hFFA2中的Ca2+通量转染子）对包括FFA3（GPR41）在内的55种其他受体/通道/转运蛋白（IC50 >10 μM）几乎没有效力。GLPG0974抑制乙酸盐诱导的人嗜中性粒细胞迁移（IC50=27 nM），并表现出体内功效（0.1或1 mg/kg胃内）对抗NSAID消炎痛/FFA2激动剂苯乙酰胺-1共同治疗诱导的十二指肠病变，具有良好的药代动力学特性和口服可用性（大鼠F=47%；口服5 mg/kg）。
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Amira Sayed Khan et al.
Cellular and molecular gastroenterology and hepatology, 15(3), 633-663 (2022-11-22)
The spontaneous preference for dietary lipids is principally regulated by 2 lingual fat taste receptors, CD36 and GPR120. Obese animals and most of human subjects exhibit low orosensory perception of dietary fat because of malfunctioning of these taste receptors. Our
Xianzhang Zeng et al.
Microbiome, 11(1), 204-204 (2023-09-12)
Aging is a significant risk factor for ischemic stroke and worsens its outcome. However, the mechanisms for this worsened neurological outcome with aging are not clearly defined. Old C57BL/6J male mice (18 to 20 months old) had a poorer neurological
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