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Rupatadine Fumarate (C007B-258439)

Catalog No.
C007B-258439
Mfr. No.
R409253-1ml
Mfr. Name
Aladdin Scientific
Qty/UOM
1
UOM
EA
Price: $117.52
List Price: $130.58

InformationRupatadine is an inhibitor ofPAFRandhistamine (H1) receptorwithKiof 550 nM and 102 nM, respectively.In vitroRupatadine inhibits both platelet-activating factor (PAF) and histamine (H1) effects through its interaction with specific

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InformationRupatadine is an inhibitor ofPAFRandhistamine (H1) receptorwithKiof 550 nM and 102 nM, respectively.In vitroRupatadine inhibits both platelet-activating factor (PAF) and histamine (H1) effects through its interaction with specific receptors. Rupatadine competitively inhibits histamine-induced guinea pig ileum contraction (pA2 = 9.29 ± 0.06) without affecting contraction induced by ACh, serotonin or leukotriene D4(LTD4). It also competitively inhibits PAF-induced platelet aggregation in washed rabbit platelets (WRP) (pA2= 6.68 ± 0.08) and in human platelet-rich plasma (HPRP) (IC50 = 0.68 μM), while not affecting ADP- or arachidonic acid-induced platelet aggregation. In another study, it is reported rupatadine and loratadine shows similar inhibitory effect on histamine and TNF-α release, whereas SR-27417A only exhibits inhibitory effect against TNF-α.In vivoRupatadine 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.). Moreover, it 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/'s duration of action is long, as assessed by the histamine- and PAF-induced increase in vascular permeability test in dogs (42 and 34% inhibition at 26 h after 1 mg/kg p.o.). Rupatadine at a dose of 100 mg/kg p.o. neither modifies spontaneous motor activity nor prolongs barbiturate-sleeping time in mice, which indicates a lack of sedative effects.Cell Datacell lines:Concentrations:up to 100 μMIncubation Time:5 minsPowder Purity:≥99%. Specification: 10mM in DMSO Molecular Formula: C26H26ClN3·C4H4O4 Molecular Weight: 532.03
UPC:
51173100
Condition:
New
Availability:
2 weeks
Weight:
0.85 Ounces
HazmatClass:
No
WeightUOM:
LB
MPN:
R409253-1ml
CAS:
182349-12-8
Product Size:
1ml

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