Zasocitinib

Zasocitinib is an inhibitor of tyrosine kinase 2 (TYK2). 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-alpha 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.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. CAS Number: 2272904-53-5. Synonyms: NDI-034858, TAK-279. Molecular Formula: C23H24N8O3. Formula Weight: 460.5. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: Acetonitrile: Soluble, DMSO: Soluble. SMILES: CO[C@H](CC1)[C@@H]1NC(C2=C3N(N=C2)C(NC)=CC(NC4=CC=CN(C5=CC=CC=N5)C4=O)=N3)=O. InChi Code: InChI=1S/C23H24N8O3/c1-24-20-12-18(27-16-6-5-11-30(23(16)33)19-7-3-4-10-25-19)29-21-14(13-26-31(20)21)22(32)28-15-8-9-17(15)34-2/h3-7,10-13,15,17,24H,8-9H2,1-2H3,(H,27,29)(H,28,32)/t15-,17-/m1/s1. InChi Key: BWINBHTTZLVXGT-NVXWUHKLSA-N.