产品
编 号：F747182
分子式：C25H27N5O7S
分子量：541.58
分子式：C25H27N5O7S
分子量：541.58
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CAS No: 1802998-75-9
产品详情
生物活性：
Filgotinib (maleate) 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. Filgotinib (maleate) can be used for rheumatoid arthritis (RA) and Crohn's disease research.
体内研究：
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.Animal Model:Rat collagen-induced arthritis (CIA)
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)
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 OrallyRat 1 mg/kg i.v.Rat 5 mg/kg Orally
Cmax or Co (ng/mL)6379201407 (28)310 (33)
Tmax (h)0.522 (0.5-5)
Area under curve:0-24 h (ng/h/mL)3471893739 (2)1681 (8)
T1/2 (h)2.51.71.63.9
Cl (L/h/kg)2.91.4
Vss (L/kg)61.8
F (%)
体外研究：
Filgotinib (maleate) (1-10 μM) inhibits Th1 and Th2 differentiation in a dose-dependent manner.
Filgotinib (maleate) 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. Filgotinib (maleate) can be used for rheumatoid arthritis (RA) and Crohn's disease research.
体内研究：
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.Animal Model:Rat collagen-induced arthritis (CIA)
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)
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 OrallyRat 1 mg/kg i.v.Rat 5 mg/kg Orally
Cmax or Co (ng/mL)6379201407 (28)310 (33)
Tmax (h)0.522 (0.5-5)
Area under curve:0-24 h (ng/h/mL)3471893739 (2)1681 (8)
T1/2 (h)2.51.71.63.9
Cl (L/h/kg)2.91.4
Vss (L/kg)61.8
F (%)
体外研究：
Filgotinib (maleate) (1-10 μM) inhibits Th1 and Th2 differentiation in a dose-dependent manner.
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