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编 号:F610765
分子式:C17H19ClN6O2
分子量:374.82
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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生物活性:
Zoniporide (CP-597396) hydrochloride hydrate is a potent and selective inhibitor of sodium-hydrogen exchanger type 1 (NHE-1). Zoniporide hydrochloride hydrate inhibits human NHE-1 (IC50=14 nM), and has >150-fold selectivity versus other NHE isoforms. Zoniporide hydrochloride hydrate potently inhibits ex vivo NHE-1-dependent swelling of human platelets (IC50=59 nM).

体内研究:
Zoniporide hydrochloride hydrate (0.25-4 mg/kg; i.v.; every hour for 2 hours) elicits a dose-dependent reduction in infarct size (ED50=0.45 mg/kg/h) in open chest anesthetized rabbits.Zoniporide exhibits moderate plasma protein binding, has a t1/2 of 1.5 hours in monkeys, and has one major active metabolite.Zoniporide hydrochloride hydrate treatment shows the AUC0-∞ and t1/2 are 0.07 μg h/mL and 0.5 hours, respectively.Animal Model:Rabbit
Dosage:0.25, 1, 4 mg/kg
Administration:Every hour for 2 hours; intravenous injection
Result:Elicited a significant dose-dependent reduction in infarct size in the anesthetized rabbit. The ED50 was 0.45 mg/kg/h.
Animal Model:Rat
Dosage:1 mg/kg
Administration:Intravenous injection(Pharmacokinetic Analysis)
Result:The AUC0-∞ and t1/2 were 0.07 μg h/mL and 0.5 hours, respectively.
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