Identification | Back Directory | [Name]
COX-1 Inhibitor II | [CAS]
304913-22-2 | [Synonyms]
ZXX277 ZXX2 77 ZXX2-77 ZXX-2-77 ZXX 2 77 COX-1 Inhibitor II | [Molecular Formula]
C13H13ClN2O2S | [MDL Number]
MFCD09907562 | [MOL File]
304913-22-2.mol | [Molecular Weight]
296.77 |
Chemical Properties | Back Directory | [Melting point ]
180-182 °C(Solv: ethyl acetate (141-78-6); hexane (110-54-3)) | [Boiling point ]
481.0±55.0 °C(Predicted) | [density ]
1.404±0.06 g/cm3(Predicted) | [pka]
1.40±0.10(Predicted) |
Hazard Information | Back Directory | [Description]
ZXX2-77 is a cyclooxygenase-1 inhibitor. | [Uses]
ZXX2-77 is a cyclooxygenase-1 (COX-1) selective inhibitor belonging to the benzenesulfonylanilide class of compounds. It is reported as a novel analgesic that does not cause gastric damage. ZXX2-77 has a weak analgesic effect but exhibits potent COX-1 inhibitory activity in vitro. The low oral absorption rate of ZXX2-77 leads to its weak analgesic effect in vivo. At a dose of 30 mg/kg, the maximum plasma concentration of ZXX2-77 (1.2 mM) did not reach its COX-1 IC50 value (3.2 mM). In contrast, its derivative ZXX2-79, although weaker in vitro COX inhibitory activity, is better absorbed, exhibits stronger analgesic effect and hardly causes gastric damage. These findings suggest that ZXX2-77 and its derivatives as COX-1 selective inhibitors may become effective analgesics that do not cause gastric damage. | [References]
[1] Effect of the Oral Absorption of Benzenesulfonanilide-Type Cyclooxygenase-1 Inhibitors on Analgesic Action and Gastric Ulcer Formation |
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