Filgotinib (GLPG0634)CAS号： 1206161-97-8分子式： C21H23N5O3S分子量： 425.5描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)
| 产品描述 | |
| 描述 |
GPLG0634 is a novel inhibitor of JAK1 and JAK2 with IC50 of 10nM and 28nM respectively. |
| 纯度 |
>98%
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| 储存/保存方法 |
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
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| 基本信息 | |
| 别名 |
GLPG0634,GLPG 0634,Filgotinib
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| 外观 |
Powder
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| 可溶性/溶解性 |
DMSO ：79 mg/mL (185.7 mM)
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| 生物活性 | |
| 靶点 |
JAK1 ,JAK2 ,TYK2 ,JAK3
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| 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.
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| In vivo(体内研究) |
Following oral administration, the JPolute 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.
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分子结构图
