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| Cas No.: | 301692-76-2 |
| Synonyms: | Polmacoxib |
| SMILES: | FC1=CC(C2=C(C3=CC=C(S(N)(=O)=O)C=C3)OC(C)(C)C2=O)=CC=C1 |
| Formula: | C18H16FNO4S |
| M.Wt: | 361.4 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | 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 (Item No. 10008672).Formulations containing polmacoxib have been used in the treatment of osteoarthritis. |