COX-2-IN-30, a benzenesulfonamide derivative, is an orally active, dual inhibitor of cyclooxygenase-2 (COX-2; IC50 = 49 nM) and cyclooxygenase-1 (COX-1; IC50 = 10.4 μM), as well as 5-lipoxygenase (5-LOX; IC50 = 2.4 μM). Additionally, it inhibits the transmembrane isoforms of human carbonic anhydrase IX and XII with nanomolar class Ki values. Demonstrating analgesic and anti-inflammatory properties, COX-2-IN-30 is devoid of acute gastric effects, avoiding ulcerogenic activity [1].

COX-2-IN-30 (Compound 7a) binds to human carbonic anhydrase (hCA) isozymes, with inhibitory constants (K i values) of 183.4 nM (hCA I), 81.4 nM (hCA II), 38.4 nM (hCA IX), and 21.6 nM (hCA XII) [1].

COX-2-IN-30 (化合物 7a) administered orally at a single dose of 10 mg/kg exhibited analgesic activity by significantly reducing the writhing frequency in mice [1]. Additionally, in the carrageenan-induced rat paw edema test, COX-2-IN-30 significantly decreased paw swelling. The compound also notably reduced the levels of pro-inflammatory cytokines TNF-α and IL-1β [1]. Furthermore, COX-2-IN-30 demonstrated safety in the gastric tissues of male albino rats at the same dosage and administration method [1].