Molecular Formula | C23H18N6O2 |
Molar Mass | 410.43 |
Storage Condition | -20°C |
In vitro study | In cell lines, GLPG0634 inhibited JAK1/JAK3/γc signaling induced by IL-2 and IL-4 and JAK1/TYK2 type II receptor signaling induced by IFN-αB2 with an IC50 in the range of 150 to 760 nM. At the cellular level, GLPG0634 is more selective for JAK/STAT signaling comprising JAK1 than JAK2 kinase. In addition, GLPG0634 also inhibits the proliferation of Th1,Th2, and Th17 cells. |
In vivo study | After oral administration, the absolute bioavailability was moderate in rats (45%) and higher in mice (100%). GLPG0634 (30 mg/kg per day (RAT);50 mg/kg twice a day (mouse)) dose-dependently reduces inflammation, cartilage, and bone degradation. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.436 ml | 12.182 ml | 24.365 ml |
5 mM | 0.487 ml | 2.436 ml | 4.873 ml |
10 mM | 0.244 ml | 1.218 ml | 2.436 ml |
5 mM | 0.049 ml | 0.244 ml | 0.487 ml |