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• 产品描述： 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

• 靶点： COX-1;COX-2;Apoptosis; COX

• 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. Cell Proliferation Assay Cell Line: A375 cells. Concentration: 100 μM.Incubation Time: 24, 48 and 72 h. Result: Caused an inhibition of cell proliferation by 38.2%, 63.2% and 66%, respectively (P < 0.001).

• 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.

• 参考文献：
  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. 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. 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. 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.

• 溶解性： soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.736 ml	13.682 ml	27.364 ml
  5 mM	0.547 ml	2.736 ml	5.473 ml
  10 mM	0.274 ml	1.368 ml	2.736 ml
  50 mM	0.055 ml	0.274 ml	0.547 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *