product name GLPG0634 analogue
Description: GLPG0634 analogue is a potent and selective JAK1 inhibitor with IC50 of 10, 28, 810, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively. In CD4+ T cells, GLPG0634 significantly reduced IL-6-induced STAT1 phosphorylation with IC50 value of 629 nM, which suggested the inhibition of JAK1. In CD33+ T cells, GLPG0634 reduced GM-CSF-induced STAT5 phosphorylation with IC50 value of 17.5 µM, suggesting the inhibition of JAK2. GLPG0634 inhibited the differentiation of Th1 and Th2 cells mediated by IL-4 and IL-12, respectively.
References: J Immunol. 2013 Oct 1;191(7):3568-77.
410.43
Formula
C23H18N6O2
CAS No.
1206101-20-3
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 0.1 mg/mL (0.24 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Following oral administration, the absolute bioavailability was moderate in rats (45%) and high in mice (∼100%). GLPG0634 (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. |
| Animal model | Rat and mouse CIA model |
| Formulation & Dosage | Dissolved in 0.5% (v/v) methylcellulose; 30 mg/kg (Rats) and 50 mg/kg (Mice); Oral administration |
| References | J Immunol. 2013 Oct 1;191(7):3568-77. |
