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Otenaproxesul

MCE China：Otenaproxesul

Brand：MedChemExpress (MCE)

Cat. No.HY-15028

CAS：1226895-20-0

Synonyms：ATB-346

Purity：98.03%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping：Room temperature in continental US; may vary elsewhere.

Description：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.

In Vitro：Otenaproxesul (100 μM) inhibits human melanoma cell proliferation by inhibiting pro-survival pathways associated with NF-B and Akt activation[2]. Otenaproxesul (100 μM) induces apoptosis of human melanoma cells[2]. 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[2].

In Vivo：Otenaproxesul exhibits anti-inflammatory properties similar to naproxen, but with substantially reduced gastrointestinal toxicity[1]. Otenaproxesul (orally, 43 μmol/kg) inhibits growth of melanoma tumors in vivo and reduce plasma levels of melanoma-associated chemokines[2]. 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[3].

IC50 & Target：COX-1 COX-2

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References：

[1]. John L Wallace, et al. Markedly reduced toxicity of a hydrogen sulphide-releasing derivative of naproxen (ATB-346). Br J Pharmacol. 2010 Mar;159(6):1236-46.  [Content Brief]

[2]. Paola De Cicco, et al. ATB-346, a novel hydrogen sulfide-releasing anti-inflammatory drug, induces apoptosis of human melanoma cells and inhibits melanoma development in vivo. Pharmacol Res. 2016 Dec;114:67-73.  [Content Brief]

[3]. Bruno Schneider Herrera, et al. The H2S-releasing naproxen derivative, ATB-346, inhibits alveolar bone loss and inflammation in rats with ligature-induced periodontitis. Med Gas Res. 2015 Feb 27;5:4.  [Content Brief]

[4]. panelEduardoEkundi-Valentim, et al. P4 Antiinflammatory and antinociceptive effects of ATB-346, a gastric sparing hydrogen sulfide-releasing naproxen, in rats with carrageenan-induced knee joint synovitis. Nitric Oxide. Volume 27, Supplement 2, 15 September 2012, Page S13.