TUL01101

Modify Date: 2023-02-06 13:24:04

TUL01101 Structure
TUL01101 structure
Common Name TUL01101
CAS Number 2411222-97-2 Molecular Weight 429.46
Density N/A Boiling Point N/A
Molecular Formula C22H25F2N5O2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of 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].

 Names

Name TUL01101

 TUL01101 Biological Activity

Description 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].
Related Catalog
Target

JAK1:3 nM (IC50)

JAK2:37 nM (IC50)

JAK3:1517 nM (IC50)

Tyk2:36 nM (IC50)

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

[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.  

 Chemical & Physical Properties

Molecular Formula C22H25F2N5O2
Molecular Weight 429.46
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