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TC JL 37

Names

[ CAS No. ]:
1258294-34-6

[ Name ]:
TC JL 37

Biological Activity

[Description]:

TCJL37 is a potent, selective, and orally bioavailable TYK2 inhibitor with a Ki of 1.6 nM. TCJL37 can be used for the research of inflammatory bowel diseases (IBD)[1].

[Related Catalog]:

Signaling Pathways >> JAK/STAT Signaling >> JAK
Signaling Pathways >> Epigenetics >> JAK
Signaling Pathways >> Stem Cell/Wnt >> JAK
Research Areas >> Inflammation/Immunology

[Target]

Tyk2:1.6 nM (Ki)


[In Vitro]

In cell-based assays, TCJL37 (Compound 37) shows IL-12 pSTAT4 EC50 of 224 nM. TCJL37 shows EC50s of 168 nM and 737 nM In human peripheral blood mononuclear cells (PBMC) and human whole blood assay, respectively[1].

[In Vivo]

TCJL37 exhibits excellent oral exposure in CD-1 mice following oral administration (100 mg/kg). TCJL37 exhibits low clearance (1.0 mL/min/kg) in rat[1].

[References]

[1]. Jun Liang, et al. Lead optimization of a 4-aminopyridine benzamide scaffold to identify potent, selective, and orally bioavailable TYK2 inhibitors. J Med Chem. 2013 Jun 13;56(11):4521-36.

Chemical & Physical Properties

[ Molecular Formula ]:
C17H11ClF2N4O2

[ Molecular Weight ]:
376.74


Related Compounds