Molecular Formula | C21H23N5O3S |
Molar Mass | 425.5 |
Density | 1.51±0.1 g/cm3(Predicted) |
Melting Point | 229 - 231°C |
Solubility | DMSO: 6.8 mg/mL |
Appearance | solid |
Color | Off-white |
pKa | 8.04±0.20(Predicted) |
Storage Condition | -20°C |
Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month. |
In vitro study | In cell lines, GLPG0634 inhibited IL-2-and IL-4-induced JAK1/JAK3/γc signaling and IFN-αB2-induced JAK1/TYK2 type II receptor signaling with IC50 values ranging from 150 to 760 nM. GLPG0634 shows higher selectivity for JAK1 kinase than JAK2 kinase in the JAK/STAT signal at the cellular level. In addition, GLPG0634 also inhibits the differentiation of Th1,Th2, and Th17 cells. |
In vivo study | After oral administration, absolute bioavailability was moderate in rats (45%) and high in mice (∼ 100). In rat and mouse CIA models, Filgotinib (30 mg/kg daily (RAT);50 mg/kg twice daily (mouse)) dose-dependently reduced inflammation, cartilage, and bone degeneration. In vivo studies with Filgotinib (GLPG0634) in DSS-treated mice showed that inhibition of JAK1 was sufficient to achieve strong efficacy in a preclinical mouse model, correlating with inhibition of STAT3 phosphorylation in inflamed colon. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.35 ml | 11.751 ml | 23.502 ml |
5 mM | 0.47 ml | 2.35 ml | 4.7 ml |
10 mM | 0.235 ml | 1.175 ml | 2.35 ml |
5 mM | 0.047 ml | 0.235 ml | 0.47 ml |