Filgotinib (maleate) 是一种选择性的，具有口服活性的JAK1抑制剂，能够有效抑制 JAK1，JAK2，JAK3 和 TYK2 的活性，IC50值分别为 10 nM，28 nM，810 nM 和 116 nM。Filgotinib (maleate) 可用于类风湿性关节炎（RA）和克罗恩病的研究。
| 生物活性 | Filgotinib (maleate) is a selective and orally activeJAK1inhibitor withIC50of 10 nM, 28 nM, 810 nM and 116 nM forJAK1,JAK2,JAK3andTYK2, respectively. Filgotinib (maleate) can be used for rheumatoid arthritis (RA) and Crohn's disease research[1][2]. |
| IC50& Target[1] | JAK1 10 nM (IC50) | JAK2 28 nM (IC50) | JAK3 810 nM (IC50) | Tyk2 116 nM (IC50) |
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体外研究
(In Vitro) | Filgotinib (maleate) (1-10 μM) inhibits Th1 and Th2 differentiation in a dose-dependent manner[1].
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体内研究
(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: | Rat collagen-induced arthritis (CIA)[1] | | Dosage: | 1 and 10 mg/kg | | Administration: | Oral administration; for 4 days | | Result: | Reduced infiltration of inflammatory cells while protecting the articular cartilage and bone. |
| Animal Model: | Rat collagen-induced arthritis (CIA)[1] | | Dosage: | 1 and 5 mg/kg | | Administration: | Oral administration and intravenous injection | | Result: | 1.19|
| Parameter (Unit) | Mouse 1 mg/kg i.v. | Mouse 5 mg/kg Orally | Rat 1 mg/kg i.v. | Rat 5 mg/kg Orally | | Cmaxor Co(ng/mL) | 637 | 920 | 1407 (28) | 310 (33) | | Tmax(h) | | 0.5 | | 22 (0.5-5) | | Area under curve:0-24 h (ng/h/mL) | 347 | 1893 | 739 (2) | 1681 (8) | | T1/2(h) | 2.5 | 1.7 | 1.6 | 3.9 | | Cl (L/h/kg) | 2.9 | | 1.4 | | | Vss(L/kg) | 6 | | 1.8 | | | F (%) | 1802998-75-9 | | 运输条件 | Room temperature in continental US; may vary elsewhere. | | 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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