产品描述: | Rupatadine (UR-12592) Fumarate is a potent, orally active and long-lasting dual PAF/H1 antagonist, with Kis of 0.55 μM and 0.1 μM, respectively. Rupatadine Fumarate can be used for the research of allergic rhinitis and urticaria |
靶点: |
H1 Receptor:0.1 μM (Ki);PAF:0.55 μM (Ki);PAFR;Autophagy;HistamineReceptor |
体内研究: |
Rupatadine Fumarate 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 Fumarate 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) Fumarate promotes the absorption of the lesions and decreased the density of lungs. |
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. |
溶解性: |
DMSO : 30 mg/mL (56.39 mM; Need ultrasonic and warming) |
保存条件: |
2-8℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
1.88 ml |
9.398 ml |
18.796 ml |
5 mM |
0.376 ml |
1.88 ml |
3.759 ml |
10 mM |
0.188 ml |
0.94 ml |
1.88 ml |
50 mM |
0.038 ml |
0.188 ml |
0.376 ml |
|
注意: |
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