GLPG0634 (Synonyms: GLPG0634)

Cell lines

THP-1 cells (ATCC TIB-202)

Preparation method

The solubility of this compound in DMSO is >21.3mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

1 μM

Applications

In THP-1 cells, GLPG0634 preferentially inhibited JAK signaling complexes containing JAK1 and also inhibited Th1 differentiation with similar potencies of 1 μM or lower.

Animal models

Male Sprague Dawley rats (180–200 g) and CD1 mice (23–25 g)

Dosage form

orally dosed as a single esophageal gavage at 5 mg/kg (dosing volume of 5 ml/kg) and i.v. dosed as a bolus via the caudal vein at 1 mg/kg (dosing volume of 5 ml/kg)

Application

GLPG0634 dose-dependently reduced inflammation, cartilage, and bone degradation in the CIA model in rats and mice with significant effect of 3 mg/kg. Protection from bone damage was evidenced by a dose-dependent reduction, with significant effect from GLPG0634 (3 mg/kg), showed a marked reduction of the infiltration of inflammatory cells while protecting the articular cartilage and bone from 1 mg/kg onward.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Van Rompaey L, Galien R, van der Aar E M., et al. Preclinical characterization of GLPG0634, a selective inhibitor of JAK1, for the treatment of inflammatory diseases. The Journal of Immunology, 2013, 191(7): 3568-3577.