Baricitinib

Baricitinib is an inhibitor of JAK1 and JAK2 (IC50s = 0.0059 and 0.0057 µM, respectively). It is selective for JAK1 and JAK2 over JAK3, TYK2, c-Met, and checkpoint kinase 2 (Chk2, IC50s = >0.4, 0.053, >10, and >1 µM, respectively). Baricitinib inhibits IL-6-induced phosphorylation of STAT3 in isolated human peripheral blood mononuclear cells (PBMCs) and rat whole blood (IC50s = 0.044 and 0.128 µM, respectively). It reduces disease severity in a type II collagen-induced mouse model of arthritis when administered at doses of 3 and 10 mg/kg. Baricitinib (4 mg/animal) also decreases lung macrophage infiltration and disease severity in rhesus monkeys infected with severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). Formulations containing baricitinib have been used in the treatment of rheumatoid arthritis.Formal Name: 1-(ethylsulfonyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]-3-azetidineacetonitrile. CAS Number: 1187594-09-7. Synonyms: INCB 028050, LY3009104. Molecular Formula: C16H17N7O2S. Formula Weight: 371.4. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 50 mg/ml, DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml, DMSO: 30 mg/ml. lambdamax: 225, 250, 310 nm. SMILES: O=S(N(C1)CC1(CC#N)N(N=C2)C=C2C3=C4C(NC=C4)=NC=N3)(CC)=O. InChi Code: InChI=1S/C16H17N7O2S/c1-2-26(24,25)22-9-16(10-22,4-5-17)23-8-12(7-21-23)14-13-3-6-18-15(13)20-11-19-14/h3,6-8,11H,2,4,9-10H2,1H3,(H,18,19,20). InChi Key: XUZMWHLSFXCVMG-UHFFFAOYSA-N.