Formulation: A solid
Formal Name: N-[(1R,2R)-2-methoxycyclobutyl]-7-(methylamino)-5-[(2-oxo[1(2H),,wbr/>2′-bipyridin]-3-yl)amino]-pyrazolo[1,5-a]pyrimidine-3-carboxamide
Purity: ≥98%
Formula Markup: C23H24N8O3
CAS Number: 2272904-53-5
Notes: Zasocitinib is an inhibitor of tyrosine kinase 2 (TYK2).{68659} It selectively binds to the TYK2 Janus homology (JH2) domain (Kd = 0.0038 nM) over the JAK1 and JAK2 JH2 domains (Kds = 4,975 and 23,000 nM, respectively). Zasocitinib inhibits the production of chemokine (C-X-C motif) ligand 10 (CXCL10) induced by IFN-α in isolated human, mouse, and rat whole blood (IC50s = 22, 347, and 91 nM, respectively). It also Inhibits IL-23-induced STAT3 phosphorylation in human CD161+CD3+ Th17 cells (IC50 = 3.7 nM). Zasocitinib (3, 10, and 30 mg/kg twice per day) decreases ankle diameter in a rat model of adjuvant-induced arthritis. It reduces the colon weight-to-length ratio and improves histology scores in a mouse model of colitis induced by an anti-CD40 antibody when administered at doses of 30 and 90 mg/kg.
English
Deutsch
