Polmacoxib

Polmacoxib is an inhibitor of cyclooxygenase 2 (COX-2) and the carbonic anhydrase subtypes I (CAI) and CAII. It inhibits COX-2 in the absence of carbonic anhydrase II with an IC50 value of 40 nM, which increases by approximately 4- and 17-fold in the presence of a CAII at a molar ratio of 1:1 and 1:5, respectively. It also inhibits CAI and CAII (IC50s = 210 and 95 nM, respectively). Polmacoxib prevents >95 and 90% of prostaglandin E2 (PGE2) production in HCA-7 and HT-29 human colon cancer cells, respectively, using concentrations of 0.01 and 0.001 µg/ml. It inhibits polyp formation in a transgenic mouse model of intestinal polyp formation and tumor growth in human colorectal carcinoma mouse xenograft models when used at a dose of 7 mg/kg. The inhibition of COX-2 and CAII by polmacoxib has the potential for fewer serious systemic adverse effects, including cardiovascular events associated with COX-2 selective inhibitors such as celecoxib (Cay-10008672). Formulations containing polmacoxib have been used in the treatment of osteoarthritis.Formal Name: 4-[3-(3-fluorophenyl)-4,5-dihydro-5,5-dimethyl-4-oxo-2-furanyl]-benzenesulfonamide. CAS Number: 301692-76-2. Molecular Formula: C18H16FNO4S. Formula Weight: 361.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 20 mg/ml, DMSO:PBS (pH 7.2)(1:8): 0.5 mg/ml, Ethanol: 5 mg/ml. lambdamax: 238, 320 nm. SMILES: FC1=CC(C2=C(C3=CC=C(S(N)(=O)=O)C=C3)OC(C)(C)C2=O)=CC=C1. InChi Code: InChI=1S/C18H16FNO4S/c1-18(2)17(21)15(12-4-3-5-13(19)10-12)16(24-18)11-6-8-14(9-7-11)25(20,22)23/h3-10H,1-2H3,(H2,20,22,23). InChi Key: IJWPAFMIFNSIGD-UHFFFAOYSA-N.