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Rupatadine
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Rupatadine图片
CAS NO:158876-82-5
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
卢帕他定
UR-12592
产品介绍
Rupatadine (UR-12592) 是一种有效的,具有口服活性的长效PAF/H1受体的双抑制剂,Ki值分别为 0.55 μM 和 0.1 μM。Rupatadine 可用于过敏性鼻炎和荨麻疹的研究。
生物活性

Rupatadine (UR-12592) is a potent, orally active and long-lasting dualPAF/H1antagonist, withKis of 0.55 μM and 0.1 μM, respectively. Rupatadine can be used for the research of allergic rhinitis and urticaria[1][2][3].

IC50& Target[1]

H1Receptor

0.1 μM (Ki)

PAF

0.55 μM (Ki)

体外研究
(In Vitro)

Rupatadine competitively inhibits histamine-induced guinea pig ileum contraction (pA2=9.29) without affecting contraction induced by ACh, serotonin or leukotriene D4 (LTD4)[1].
Rupatadine competitively inhibits PAF-induced platelet aggregation in washed rabbit platelets (WRP) (pA2=6.68) and in human platelet-rich plasma (HPRP) (IC50=0.68 μM), while not affecting ADP- or arachidonic acid-induced platelet aggregation[1].
Rupatadine (0.1-30 μM) inhibits TNF-α secretion in a concentration-dependent manner, with maximum values of 92.5%[2].

体内研究
(In Vivo)

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.)[1].
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.)[1].
Rupatadine (6 mg/kg) promotes the absorption of the lesions and decreased the density of lungs[3].

Animal Model:Male C57BL/6J mice (18 g, 6-8 wk)[3]
Dosage:1.5, 3, 6 mg/kg
Administration:Oral gavage once a day
Result:Markedly decreased the BLM-enhanced inflammatory scores and lung index.
Clinical Trial
分子量

415.96

Formula

C26H26ClN3

CAS 号

158876-82-5

中文名称

卢帕他定

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.