产品
编 号：F752218
分子式：C22H25F2N5O2
分子量：429.46
分子式：C22H25F2N5O2
分子量：429.46
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CAS No: 2411222-97-2
产品详情
生物活性：
TUL01101 is a potent, selective and orally active JAK1 inhibitor, with an IC50s of 3, 37, 1517 and 36 nM for JAK1, JAK2, JAK3, and TYK2, respectively. TUL01101 can be used for the research of rheumatoid arthritis.
体内研究：
TUL01101 (1-30 mg/kg; p.o. twice daily for 14 d) inhibits rheumatoid arthritis in the rat adjuvant-induced arthritis (AIA) model.TUL01101 (15 mg/kg; p.o. twice daily for 14 d) inhibits rheumatoid arthritis in collagen-induced arthritis models.TUL01101 (15 mg/kg; p.o.) exhibits T1/2 of 2.01 h, Cmax of 5105 nM, and oral bioavailability of 38.1% in mice.TUL01101 (10 mg/kg; p.o.) exhibits T1/2 of 3.06 h, Cmax of 4965 nM, and oral bioavailability of 121% in rats.TUL01101 (5 mg/kg; p.o.) exhibits T1/2 of 4.49 h, Cmax of 2750 nM, and oral bioavailability of 106.5% in dogs.Animal Model:Rat adjuvant-induced arthritis (AIA) model
Dosage:1, 3, 10, 30 mg/kg
Administration:Orally administered twice daily for 14 days
Result:Decreased the incidence in a dose-dependent manner.
体外研究：
TUL01101 (pretreatment for 1 h) inhibits cytokine-induced pSTAT in human whole blood assay.
TUL01101 is a potent, selective and orally active JAK1 inhibitor, with an IC50s of 3, 37, 1517 and 36 nM for JAK1, JAK2, JAK3, and TYK2, respectively. TUL01101 can be used for the research of rheumatoid arthritis.
体内研究：
TUL01101 (1-30 mg/kg; p.o. twice daily for 14 d) inhibits rheumatoid arthritis in the rat adjuvant-induced arthritis (AIA) model.TUL01101 (15 mg/kg; p.o. twice daily for 14 d) inhibits rheumatoid arthritis in collagen-induced arthritis models.TUL01101 (15 mg/kg; p.o.) exhibits T1/2 of 2.01 h, Cmax of 5105 nM, and oral bioavailability of 38.1% in mice.TUL01101 (10 mg/kg; p.o.) exhibits T1/2 of 3.06 h, Cmax of 4965 nM, and oral bioavailability of 121% in rats.TUL01101 (5 mg/kg; p.o.) exhibits T1/2 of 4.49 h, Cmax of 2750 nM, and oral bioavailability of 106.5% in dogs.Animal Model:Rat adjuvant-induced arthritis (AIA) model
Dosage:1, 3, 10, 30 mg/kg
Administration:Orally administered twice daily for 14 days
Result:Decreased the incidence in a dose-dependent manner.
体外研究：
TUL01101 (pretreatment for 1 h) inhibits cytokine-induced pSTAT in human whole blood assay.
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