Bioactivity | Filgotinib (maleate) is a selective and orally active JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM and 116 nM for JAK1, JAK2, JAK3 and TYK2, respectively. Filgotinib (maleate) can be used for rheumatoid arthritis (RA) and Crohn's disease research[1][2]. |
Invitro | Filgotinib (maleate) (1-10 μM) inhibits Th1 and Th2 differentiation in a dose-dependent manner[1]. |
In Vivo | Filgotinib (maleate) (1-10 mg/mL; p.o. and i.v.; Rat collagen-induced arthritis) exhibits good pharmacokinetic profiles and reduces paw swelling, bone and cartilage degradation and levels ofinflammatory cytokines[1]. Animal Model: |
Name | Filgotinib maleate |
CAS | 1802998-75-9 |
Formula | C25H27N5O7S |
Molar Mass | 541.58 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Van Rompaey L, et, al. Preclinical characterization of GLPG0634, a selective inhibitor of JAK1, for the treatment of inflammatory diseases. J Immunol. 2013 Oct 1;191(7):3568-77. [2]. Labetoulle R, et al. Filgotinib for the treatment of Crohn's disease. Expert Opin Investig Drugs. 2018 Mar;27(3):295-300. |