产品
编 号:F082275
分子式:C21H19NO3S
分子量:365.45
产品类型
结构图
CAS No: 1226895-20-0
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生物活性:
Otenaproxesul (ATB-346), an orally active non-steroidal anti-inflammatory drug (NSAID), inhibits cyclooxygenase-1 and 2 (COX-1 and 2). Otenaproxesul possesses antiinflammatory and antinociceptive activities.
体内研究:
Otenaproxesul exhibits anti-inflammatory properties similar to naproxen, but with substantially reduced gastrointestinal toxicity.Otenaproxesul (orally, 43 μmol/kg) inhibits growth of melanoma tumors in vivo and reduce plasma levels of melanoma-associated chemokines.Otenaproxesul (orally, 16 mg/kg) results in significant inhibition of bone defect and other histological characteristics (such as flatness of the gingival epithelium, chronic inflammatory cell infiltration and loss of connective tissue in the gingival papillae). Otenaproxesul inhibits the increase of gingival IL-1β and IL-6 secondary to periodontitis, but IL-10 is unaffected.Animal Model:Male, Wistar rats (200-225 g).
Dosage:30, 60, 120 and 2740 μmol/kg.
Administration:Orally once.
Result:Inhibited PGE2 levels.Suppressed TXB2 synthesis.
Animal Model:Male, Wistar rats (200-225 g).
Dosage:4 μmol/kg.
Administration:Orally twice daily, on days 7 to 21.
Result:Significantly reduced paw oedema at days 14 and 21 (*P < 0.05 vs. the vehicle-treated group).Caused markedly less gastric damage at all doses tested than naproxen.
体外研究:
Otenaproxesul (100 μM) inhibits human melanoma cell proliferation by inhibiting pro-survival pathways associated with NF-B and Akt activation.Otenaproxesul (100 μM) induces apoptosis of human melanoma cells.Otenaproxesul (100 M) causes inhibition of IkB degradation and of NF-kB nuclear translocation as demonstrated by a reduction in band intensity of the p65 subunit in A375 cells.