Filgotinib
CAS No. : 1206161-97-8
(Synonyms: GLPG0634)
| Size | Price | Stock |
|---|---|---|
| 5mg | $92 | In-stock |
| 10mg | $145 | In-stock |
| 25mg | $238 | In-stock |
| 50mg | $320 | In-stock |
| 100mg | $420 | In-stock |
| 500mg | $1280 | In-stock |
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| Cat. No. : | HY-18300 |
| M.Wt: | 425.50 |
| Formula: | C21H23N5O3S |
| Purity: | >98 % |
| Solubility: | H2O : < 0.1 mg/mL;DMSO : 25 mg/mL (ultrasonic) |
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].
IC50 & Target:IC50: 10 nM (JAK1), 28 nM (JAK2), 810 nM (JAK3), 116 nM (Tyk2)
In Vitro:Filgotinib (0.1, 1 and 10 μM) inhibits the differentiation of Th2 cells and Th1 cells in a dose-dependent manner[1].
In Vivo:Filgotinib (0.1, 0.3, 1, 3, 10 and 30 mg/kg, i.g.; once daily for 15 days) produces dose-dependent bone damage protection and prevents the development of inflammation in a rat model of collagen-induced arthritis[1].
Pharmacokinetic analysis of GLPG0634 in mice[1]
| Route | Dose (mg/kg) | C0 or C0 (ng/mL) | Tmax (h) | T1/2 (h) | Cl (L•h/kg) | Vss (L/kg) | F (%) |
| i.v. | 1 | 637 | / | 2.5 | 2.9 | 6 | / |
| p.o. | 5 | 920 | 0.5 | 1.7 | / | / | 100 |