1206161-97-8
Chemical Structure
Filgotinib
Synonym(s): GLPG0634
- CAS No.: 1206161-97-8
- Formula:C21H23N5O3S
- Molecular Weight:425.50
IUPAC Name: N-(5-(4-((1,1-dioxidothiomorpholino)methyl)phenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl)cyclopropanecarboxamide
InChIKey: RIJLVEAXPNLDTC-UHFFFAOYSA-N
SMILES: O=C(C1CC1)NC2=NN3C(C4=CC=C(CN5CCS(CC5)(=O)=O)C=C4)=CC=CC3=N2
Biological Activity: Filgotinib (GLPG0634) is a selective, orally available JAK1 inhibitor with anti-inflammatory and antiviral activities. Filgotinib 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 also inhibits HIV-1 driven gene transcription and reduces proliferation of HIV-1 infected cells. Filgotinib can be used in the study of rheumatoid arthritis and inflammatory bowel disease[1][2][3].
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Filgotinib | 99.77% | Filgotinib (GLPG0634) is a selective, orally available JAK1 inhibitor with anti-inflammatory and antiviral activities. Filgotinib 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 also inhibits HIV-1 driven gene transcription and reduces proliferation of HIV-1 infected cells. Filgotinib can be used in the study of rheumatoid arthritis and inflammatory bowel disease. | ||||||||||||||||||||
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Filgotinib (Standard) | 99.56% | Filgotinib (Standard) is the analytical standard of Filgotinib. This product is intended for research and analytical applications. Filgotinib (GLPG0634) 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. | ||||||||||||||||||||
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Filgotinib-d4 | Filgotinib-d4 is the deuterium labeled Filgotinib. 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. | |||||||||||||||||||||
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Similarity Score 0.88
HY-18300AFilgotinib maleate -
Similarity Score 0.76
HY-W394903GS-829845 -
Similarity Score 0.71
HY-16755Solcitinib -
Similarity Score 0.66
HY-46262JAK-IN-15 -
Similarity Score 0.65
HY-13961GLPG0634 analog -
Similarity Score 0.64
HY-139423JAK1-IN-8 -
Similarity Score 0.56
HY-181929RAI-20 -
Similarity Score 0.53
HY-124283LEI-101 free base -
Similarity Score 0.52
HY-124283ALEI-101 -
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References
- [1]. Van Rompaey L, et al. Preclinical characterization of GLPG0634, a selective inhibitor of JAK1, for the treatment of inflammatory diseases. J Immunol. 2013, 191(7), 3568-3577. [Content Brief]
- [2]. Menet CJ, et al. Triazolopyridines as Selective JAK1 Inhibitors: From Hit Identification to GLPG0634. J Med Chem. 2014 Nov 17. [Content Brief]
- [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. [Content Brief]
