Rupatadine Fumarate

Research use only, not for human use.

Rupatadine is an inhibitor of PAFR and histamine (H1) receptor with Ki of 550 nM and 102 nM, respectively.

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