产品信息
抗原名称
JAK1 ,JAK2 ,TYK2 ,JAK3
商品描述
GPLG0634 is a novel inhibitor of JAK1 and JAK2 with IC50 of 10nM and 28nM respectively.
分子量
425.5
纯度
>98%
可溶性
DMSO ：79 mg/mL (185.7 mM)
外观
Powder
In vitro(体外研究)
In cell lines, GLPG0634 inhibits IL-2- and IL-4-induced JAK1/JAK3/γc signaling and IFN-αB2-induced JAK1/TYK2 type II receptor signaling with IC50 ranged from 150 to 760 nM. GLPG0634 shows higher selectivity for JAK/STAT signaling involving JAK1 than JAK2 kinase in a cellular context. Besides, GLPG0634 also inhibits the differentiation of Th1, Th2, and Th17 cells.
In vivo(体内研究)
Following oral administration, the absolute bioavailability is moderate in rats (45%) and high in mice (∼100%). Filgotinib (30 mg/kg daily (Rats); 50 mg/kg twice daily (Mice)) dose-dependently reduces inflammation, cartilage, and bone degradation in the CIA model in rats and mice. Filgotinib (GLPG0634) in DSS-treated mice demonstrates that inhibition of JAK1 is sufficient for achieving strong efficacy in pre-clinical mouse model, correlated to the inhibition of STAT3 phosphorylation in the inflamed colon.
背景
别名
GLPG0634,GLPG 0634,Filgotinib
分子式
C21H23N5O3S
CAS号
1206161-97-8
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
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