目錄:MedChemExpress LLC>>生化試劑>> Rupatadine | MCE
CAS | 158876-82-5 | 分子量 | 415.96 |
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分子式 | C??H??ClN? | 供貨周期 | 現(xiàn)貨 |
貨號 | HY-13511 | 應用領域 | 醫(yī)療衛(wèi)生,化工,生物產(chǎn)業(yè),制藥 |
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CAS No. : 158876-82-5
產(chǎn)品活性: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.
研究領域:GPCR/G Protein | Neuronal Signaling | Immunology/Inflammation | Autophagy
作用靶點:Histamine Receptor | Autophagy
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).
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.
Rupatadine (0.1-30 μM) inhibits TNF-α secretion in a concentration-dependent manner, with maximum values of 92.5%.
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.).
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.
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