Iguratimod

Iguratimod is a disease-modifying antirheumatic drug (DMARD) and COX-2 inhibitor (IC50 = 7.7 µg/ml). It is selective for COX-2 over COX-1 (IC50 = >300 µg/ml) but also inhibits the tautomerase activity of macrophage migration inhibitory factor (MIF, IC50 = 6.81 µM). Iguratimod (1-10 µM) inhibits osteoclastogenesis and bone resorption of isolated mouse bone marrow-derived macrophages stimulated with macrophage colony-stimulating factor (M-CSF) and RANKL, as well as prevents bone loss in ovariectomized mice. It decreases disease severity in a rat model of collagen-induced arthritis when administered alone or in combination with methotrexate (Cay-13960). Iguratimod (12.5 mg/kg) also decreases disease severity in a MOG35-55 mouse model of experimental autoimmune encephalomyelitis (EAE) when administered in combination with dexamethasone (Cay-11015). Formulations containing iguratimod have been used in the treatment of rheumatoid arthritis.Formal Name: N-[3-(formylamino)-4-oxo-6-phenoxy-4H-1-benzopyran-7-yl]-methanesulfonamide. CAS Number: 123663-49-0. Synonyms: IGU, T-614. Molecular Formula: C17H14N2O6S. Formula Weight: 374.4. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 14 mg/ml, DMSO: 16 mg/ml, PBS (pH 7.2): 0.25 mg/ml. lambdamax: 257, 264 nm. SMILES: O=CNC1=COC2=CC(NS(=O)(C)=O)=C(C=C2C1=O)OC3=CC=CC=C3. InChi Code: InChI=1S/C17H14N2O6S/c1-26(22,23)19-13-8-15-12(17(21)14(9-24-15)18-10-20)7-16(13)25-11-5-3-2-4-6-11/h2-10,19H,1H3,(H,18,20). InChi Key: ANMATWQYLIFGOK-UHFFFAOYSA-N.