Rupatadine Fumarate

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Rupatadine 是 PAFR 和组胺 (H1) 受体的抑制剂，Ki 分别为 550 nM 和 102 nM。

Rupatadine is an inhibitor of PAFR and histamine (H1) receptor with Ki of 550 nM and 102 nM, respectively.(In Vitro):Rupatadine Fumarate competitively inhibits histamine-induced guinea pig ileum contraction (pA2=9.29) without affecting contraction induced by ACh, serotonin or leukotriene D4 (LTD4).Rupatadine Fumarate 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) Fumarate inhibits TNF-α secretion in a concentration-dependent manner, with maximum values of 92.5%.(In Vivo):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.

Rupatadine Fumarate competitively inhibits histamine-induced guinea pig ileum contraction (pA2=9.29) without affecting contraction induced by ACh, serotonin or leukotriene D4 (LTD4). Rupatadine Fumarate 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) Fumarate inhibits TNF-α secretion in a concentration-dependent manner, with maximum values of 92.5%.

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. 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.

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GPCR/G Protein

Histamine Receptor

H1 receptor| PAFR

Inflammation/Immunology

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182349-12-8

532.03

C26H26ClN3·C4H4O4

>98% (HPLC)

Ethanol: 13 mg/mL (24.43 mM); DMSO: 9 mg/mL (16.91 mM)

CC1=CC(=CN=C1)CN2CCC(=C3C4=C(CCC5=C3N=CC=C5)C=C(C=C4)Cl)CC2.C(=C/C(=O)O)\C(=O)O

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(-20℃)

With Ice Pack

≥ 2 years