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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)[1][2]. | [in vivo]
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[1].
Zoniporide exhibits moderate plasma protein binding, has a t1/2 of 1.5 hours in monkeys, and has one major active metabolite[1].
Zoniporide hydrochloride hydrate treatment shows the AUC0-∞ and t1/2 are 0.07 μg h/mL and 0.5 hours, respectively[2]. | Animal Model: | Rabbit[1] | | 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[2] | | 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. |
| [storage]
Store at -20°C | [References]
[1] Tracey WR, et al. Zoniporide: a potent and selective inhibitor of the human sodium-hydrogen exchanger isoform 1 (NHE-1). Cardiovasc Drug Rev. 2003 Spring;21(1):17-32. DOI:10.1111/j.1527-3466.2003.tb00103.x
[2] Guzman-Perez A, et al. Discovery of zoniporide: a potent and selective sodium-hydrogen exchanger type 1 (NHE-1) inhibitor with high aqueous solubility. Bioorg Med Chem Lett. 2001 Mar 26;11(6):803-7. DOI:10.1016/s0960-894x(01)00059-2 |
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