TUL01101

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[1].

Signaling Pathways >> JAK/STAT Signaling >> JAK

Signaling Pathways >> Epigenetics >> JAK

Signaling Pathways >> Stem Cell/Wnt >> JAK

Research Areas >> Inflammation/Immunology

JAK1:3 nM (IC50)

JAK2:37 nM (IC50)

JAK3:1517 nM (IC50)

Tyk2:36 nM (IC50)

TUL01101 (pretreatment for 1 h) inhibits cytokine-induced pSTAT in human whole blood assay[1].

TUL01101 (1-30 mg/kg; p.o. twice daily for 14 d) inhibits rheumatoid arthritis in the rat adjuvant-induced arthritis (AIA) model[1]. TUL01101 (15 mg/kg; p.o. twice daily for 14 d) inhibits rheumatoid arthritis in collagen-induced arthritis models[1]. 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[1]. TUL01101 (10 mg/kg; p.o.) exhibits T1/2 of 3.06 h, Cmax of 4965 nM, and oral bioavailability of 121% in rats[1]. 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[1]. Animal Model: Rat adjuvant-induced arthritis (AIA) model[1] Dosage: 1, 3, 10, 30 mg/kg Administration: Orally administered twice daily for 14 days Result: Decreased the incidence in a dose-dependent manner.

[1]. Zhou S, et, al. Identification of TUL01101: A Novel Potent and Selective JAK1 Inhibitor for the Treatment of Rheumatoid Arthritis. J Med Chem. 2022 Dec 22;65(24):16716-16740.