l General Information |
Product Name | Filgotinib (GLPG0634) |
General description | Filgotinib (GLPG0634) is a selective JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively. |
Synonym | N-[5-[4-[(1,1-dioxo-1,4-thiazinan-4-yl)methyl]phenyl]-[1,2,4]triazolo[1,5-a]pyridin-2-yl]cyclopropanecarboxamide |
Purity | ≥98.5%(HPLC) | CAS Number | 1206161-97-8 |
Formula | C21H23N5O3S | Molecular Weight | 425.5 |
Suitability | BioReagent, suitable for cell culture, etc. |
l Physical and Chemical Information |
Appearance | Solid |
Solubility(25°C) | DMSO | ≥50mg/ml |
Ethanol | Insoluble |
Water | Very slightly soluble |
l Biological Information |
Biochem/Physiol
Actions | Filgotinib is an orally bioavailable inhibitor of the tyrosine kinase Janus kinase 1 (JAK1), with potential anti-inflammatory and immunomodulating activities. Upon oral administration, filgotinib specifically targets, binds to, and inhibits the phosphorylation of JAK1, which interferes with JAK/STAT (signal transducer and activator of transcription)-dependent signaling. As JAK1 mediates signaling of many pro-inflammatory cytokines, JAK1 inhibition prevents cytokine signaling and activity in many inflammatory and immune-mediated processes and leads to a decrease in inflammation and activation of certain immune cells. JAK1 plays a key role in the signaling and activity of many cytokines and growth factors and is often dysregulated in a variety of autoimmune and inflammatory diseases, as well as some malignancies. |
l Storage |
Storage temp. | -20°C |
l Precautions and Disclaimer |
This product is for R&D use only, not for drug, household, or other uses. |
l References |
1. http://www.drugbank.ca 2. https://ncit.nci.nih.gov 3. https://www.ncbi.nlm.nih.gov |
