产品
编 号：F755095
分子式：C17H21F2N7O
分子量：377.39
分子式：C17H21F2N7O
分子量：377.39
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CAS No: 2734918-37-5
产品详情
生物活性：
JAK1/TYK2-IN-3 is a potent, selective and orally active dual TYK2/JAK1 inhibitor with IC50 values of 6 and 37 nM, respectively. JAK1/TYK2-IN-3 also shows selectively relative to JAK2 (IC50=140 nM) and JAK3 (IC50=362 nM). JAK1/TYK2-IN-3 shows anti-inflammatory effect by regulating the expression of related TYK2/JAK1-regulated genes, as well as the formation of Th1, Th2, and Th17 cells.
体内研究：
JAK1/TYK2-IN-3 (10, 20, 30 mg/kg; p.o.; twice a day for 12 days) shows a good therapeutic effect on ulcerative colitis (UC).JAK1/TYK2-IN-3 (5 mg/kg, p.o.) shows 23.7% oral bioavailability in rats.Pharmacokinetic Parameters of JAK1/TYK2-IN-3 in male Sprague-Dawley rats.compddose(mg/kg) AdministrationCmax(ng/mL) Cl (Lh-1kg-1) T1/2(h) AUC0-t(ng·h/mL)F (%)
485 mg/kgp.o.400.4±55.311.3±5.22.4±2.1440.9±157.023.7
Animal Model:6-8 weeks, 270-325g male Sprague-Dawley rats
Dosage:5 mg/kg
Administration:p.o.
Result:Showed 23.7% oral bioavailability in rats.
Animal Model:Six-eight week old male C57BL/6 mice, 20-22 g (2.5% dextran sulfate sodium (DSS)-induced acute UC mouse model)
Dosage:10, 20, 30 mg/kg
Administration:p.o., twice a day, 12 days
Result:Improved the infiltration of inflammatory factors and reduced the damage caused by DSS.
体外研究：
JAK1/TYK2-IN-3 (compound 48) (10, 20, 30 mg/kg) shows anti-inflammatory effect by regulating the formation of Th1, Th2, Th17 cells.JAK1/TYK2-IN-3 (10, 20, 30 mg/kg) inhibits the NF-κB signaling pathway by inhibits the JAK-STAT pathway, thereby reducing the inflammatory response in ulcerative colitis (UC) mice.JAK1/TYK2-IN-3 (10, 20, 30 mg/kg) dose-dependently inhibits the mRNA expression of TNF-α, IL-1β, IL-12, IL-17A, IL-22, IFN-α, and IFN-β.
JAK1/TYK2-IN-3 is a potent, selective and orally active dual TYK2/JAK1 inhibitor with IC50 values of 6 and 37 nM, respectively. JAK1/TYK2-IN-3 also shows selectively relative to JAK2 (IC50=140 nM) and JAK3 (IC50=362 nM). JAK1/TYK2-IN-3 shows anti-inflammatory effect by regulating the expression of related TYK2/JAK1-regulated genes, as well as the formation of Th1, Th2, and Th17 cells.
体内研究：
JAK1/TYK2-IN-3 (10, 20, 30 mg/kg; p.o.; twice a day for 12 days) shows a good therapeutic effect on ulcerative colitis (UC).JAK1/TYK2-IN-3 (5 mg/kg, p.o.) shows 23.7% oral bioavailability in rats.Pharmacokinetic Parameters of JAK1/TYK2-IN-3 in male Sprague-Dawley rats.compddose(mg/kg) AdministrationCmax(ng/mL) Cl (Lh-1kg-1) T1/2(h) AUC0-t(ng·h/mL)F (%)
485 mg/kgp.o.400.4±55.311.3±5.22.4±2.1440.9±157.023.7
Animal Model:6-8 weeks, 270-325g male Sprague-Dawley rats
Dosage:5 mg/kg
Administration:p.o.
Result:Showed 23.7% oral bioavailability in rats.
Animal Model:Six-eight week old male C57BL/6 mice, 20-22 g (2.5% dextran sulfate sodium (DSS)-induced acute UC mouse model)
Dosage:10, 20, 30 mg/kg
Administration:p.o., twice a day, 12 days
Result:Improved the infiltration of inflammatory factors and reduced the damage caused by DSS.
体外研究：
JAK1/TYK2-IN-3 (compound 48) (10, 20, 30 mg/kg) shows anti-inflammatory effect by regulating the formation of Th1, Th2, Th17 cells.JAK1/TYK2-IN-3 (10, 20, 30 mg/kg) inhibits the NF-κB signaling pathway by inhibits the JAK-STAT pathway, thereby reducing the inflammatory response in ulcerative colitis (UC) mice.JAK1/TYK2-IN-3 (10, 20, 30 mg/kg) dose-dependently inhibits the mRNA expression of TNF-α, IL-1β, IL-12, IL-17A, IL-22, IFN-α, and IFN-β.
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