| 货号 | 16234-25mg |
| 描述 | ATB-346 is a non-steroidal anti-inflammatory drug (NSAID), derived from naproxen but coupled to an H2S-releasing moiety.1 At 30 µmol/kg in rats, it suppressed COX and gastric PGE2 synthesis to the same level as naproxen but reduced COX-2 expression and accelerated recovery in a rat spinal cord injury model.2 It also provided enhanced anti-inflammatory and antinociceptive activity over naproxen in a rat model of arthritis.3 ATB-346 does not induce gastrointestinal toxicity and, in contrast to other NSAIDs, it accelerated healing of pre-existing gastric ulcers.4 Studies of ATB-346 have shown promising results in vitro and in animal models of melanoma and intestinal tumorigenesis.5,6 A Phase I clinical trial in Canada did not find any significant gastrointestinal, cardiovascular, renal, or hematological findings across dose ranges in healthy adults (25 mg–2,000 mg once/d).7 A Phase II trial in Canada is ongoing for patients with osteoarthritis of the knee. |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Fiorucci, S. and Santucci, L. Hydrogen sulfide-based therapies: Focus on H2S releasing NSAIDs. Inflamm. Allergy Drug Targets 133-140 (2011). 2.Campolo, M.,Esposito, E.,Ahmad, A., et al. A hydrogen sulfide-releasing cyclooxygenase inhibitor markedly accelerates recovery from experimental spinal cord injury. FASEB J. 27(11), 4489-1199 (2013). 3.Dief, A.E.,Mostafa, D.K.,Sharara, G.M., et al. Hydrogen sulfide releasing naproxen offers better anti-inflammatory and chondroprotective effect relative to naproxen in a rat model of zymosan induced arthritis. Eur. Rev. Med. Pharmacol. Sci. 19(8), 1537-1546 (2015). 4.Wallace, J.L.,Caliendo, G.,Santagada, V., et al. Markedly reduced toxicity of a hydrogen sulphide-releasing derivative of naproxen (ATB-346). Br. J. Pharmacol. 159(6), 1236-1246 (2010). 5.De Cicco, P.,Panza, E.,Ercolano, G., 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. 114, 67-73 (2016). 6.Paul-Clark, M.J.,Elsheikh, W.,Kikby, N., et al. Profound Chemopreventative Effects of a Hydrogen Sulfide-Releasing NSAID in the APCMin/+ Mouse Model of Intestinal Tumorigenesis. PLoS One 11(2), e0147289 (2016). 7.Wallace, J.L. THU0474 a phase 1 clinical trial of ATB-346, a gastrointestinal-ssafe nonsteroidal anti-inflammatory drug. Ann. Rheum. Dis. 74 (Suppl 2), 371-372 (2015). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 365.5 |
| 分子式 | C21H19NO3S |
| CAS号 | 1226895-20-0 |
| 稳定性 | ≥ 2 years |
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