polmacoxib

Polmacoxib (CG 100649) is a first-in-class NSAID drug candidate, is a dual inhibitor of carbonic anhydrase (CA) and COX-2. Polmacoxib inhibits premalignant and malignant colorectal lesions in mouse models, partly through inhibiting tumor cell proliferation.

Anti-inflammatory agent 67 (compound 7a) is a dual inhibitor targeting Carbonic Anhydrase and COX-2, and is a sulfonamide derivative of Polmacoxib. It exhibits anti-inflammatory and analgesic properties. The IC50 values for COX-1 and COX-2 are 10.4 μM and 50 nM, respectively. The Ki values for binding to various Carbonic Anhydrase isoforms are 48.3 nM (CA I), 42.2 nM (CA II), 52.3 nM (CA IX), and 13.3 nM (CA XII).

Anti-inflammatory agent 68 (compound 7b) is a dual inhibitor that targets Carbonic Anhydrase and COX-2, and is a sulfonamide derivative of Polmacoxib, exhibiting anti-inflammatory and analgesic properties. The IC50 values of Anti-inflammatory agent 68 for COX-1 and COX-2 are 12.6 μM and 60 nM, respectively. It binds to different Carbonic Anhydrase isoforms with Ki values of 52.6 nM (CA I), 79.1 nM (CA II), 58.1 nM (CA IX), and 17.2 nM (CA XII).