Filgotinib (maleate)

Filgotinib maleate (GLPG0634 maleate) is a selective, orally available JAK1 inhibitor with anti-inflammatory and antiviral activities. Filgotinib maleate can effectively inhibit the activities of JAK1, JAK2, JAK3 and TYK2 with IC50 values of 10 nM, 28 nM, 810 nM and 116 nM, respectively. Filgotinib maleate also inhibits HIV-1 driven gene transcription and reduces proliferation of HIV-1 infected cells. Filgotinib maleate can be used in the study of rheumatoid arthritis and inflammatory bowel disease[1][2][3].

Product Specifications

CAS Number

[1802998-75-9]

Product Name Alternative

GLPG0634 (maleate)

UNSPSC

12352005

Hazard Statement

H360, H373

Target

HIV; JAK

Type

Reference compound

Related Pathways

Anti-infection; Epigenetics; JAK/STAT Signaling; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/filgotinib-maleate.html

Purity

99.88

Solubility

DMSO : 35 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

OC(/C=C\C(O)=O)=O.O=C(C1CC1)NC2=NN3C(C4=CC=C(C=C4)CN5CCS(=O)(CC5)=O)=CC=CC3=N2

Molecular Formula

C25H27N5O7S

Molecular Weight

541.58

Precautions

H360, H373

References & Citations

[2]Labetoulle R, et al. Filgotinib for the treatment of Crohn's disease. Expert Opin Investig Drugs. 2018 Mar;27 (3) :295-300.|[3]Yeh, et al. "Filgotinib suppresses HIV-1–driven gene transcription by inhibiting HIV-1 splicing and T cell activation." The Journal of Clinical Investigation 130.9 (2020) : 4969-4984.|[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.