| 产品描述： | Rupatadine (UR-12592) is a potent, orally active and long-lasting dual PAF/H1 antagonist, with Kis of 0.55 μM and 0.1 μM, respectively. Rupatadine can be used for the research of allergic rhinitis and urticaria |
| 靶点： |
H1 Receptor:0.1 μM (Ki);PAF:0.55 μM (Ki) |
| 体内研究： |
Rupatadine blocks histamine- and PAF-induced effects in vivo, such as hypotension in rats (ID50=1.4 and 0.44 mg/kg i.v., respectively) and bronchoconstriction in guinea pigs (ID50=113 and 9.6 μg/kg i.v.). Rupatadine potently inhibits PAF-induced mortality in mice (ID50=0.31 and 3.0 mg/kg i.v. and p.o., respectively) and endotoxin-induced mortality in mice and rats (ID50=1.6 and 0.66 mg/kg i.v.). Rupatadine (6 mg/kg) promotes the absorption of the lesions and decreased the density of lungs. Animal Model: Male C57BL/6J mice (18 g, 6-8 wk) Dosage: 1.5, 3, 6 mg/kg Administration: Oral gavage once a day Result: Markedly decreased the BLM-enhanced inflammatory scores and lung index. |
| 参考文献： |
1. Merlos M, et al. Rupatadine, a new potent, orally active dual antagonist of histamine and platelet-activating factor (PAF). J Pharmacol Exp Ther. 1997 Jan;280(1):114-21. 2. Queralt M, et al. In vitro inhibitory effect of rupatadine on histamine and TNF-alpha release from dispersed canine skin mast cells and the human mast cell line HMC-1. Inflamm Res. 2000 Jul;49(7):355-60. 3. Lv XX, et al. Rupatadine protects against pulmonary fibrosis by attenuating PAF-mediated senescence in rodents. PLoS One. 2013 Jul 15;8(7):e68631. |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.404 ml |
12.02 ml |
24.041 ml |
| 5 mM |
0.481 ml |
2.404 ml |
4.808 ml |
| 10 mM |
0.24 ml |
1.202 ml |
2.404 ml |
| 50 mM |
0.048 ml |
0.24 ml |
0.481 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京