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编 号:F762358
分子式:C17H23N5O4S
分子量:393.46
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生物活性:
JAK3-IN-9 is an orally active JAK3 inhibitor with IC50 value of 1.7 nM. JAK3-IN-9 is highly selective to the JAK3 signal path. JAK3-IN-9 is lowly toxic with high oral bioavailability, shows good anti-arthritis activity. JAK3-IN-9 can be used in autoimmune disease research.

体内研究:
JAK3-IN-9 (compound 11i) (Female Lewis rats; 3, 10 and 30 mg/kg; Oral gavage once daily for 20 days) can selectively inhibit JAK3 cytokine signaling in the primary cells.JAK3-IN-9 (Male DBA1j of 8 to 12-weeks old mice; 1mg/kg, Intravenous injection, Single administration) shows high AUC of 2104 μg/ml, extends t1/2 to 2.56 h and good oral bioavailability of 48%.JAK3-IN-9 (30 mg/kg; Oral gavage once daily for 20 days) suppress paw swelling in a dose-dependent manner with ED50 value of 10 mg/kg.Animal Model: Male DBA1j (8 to 12-weeks old) mice; Female Lewis rats.
Dosage:1, 3, 10 and 30 mg/kg
Administration:I.V, Single administration; IG, once daily for 20 days.
Result:Showed anti-arthritis activity in the CIA mice model.

体外研究:
JAK3-IN-9 (compound 11i) shows high selective inhibition of JAK3 with IC50 value of 1.7 nM .
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