Zoniporide hydrochloride hydrate (C09-1185-882)

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 ( IC 50 =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 (IC 50 =59 nM)In VivoZoniporide hydrochloride hydrate (0.25-4 mg/kg; i.v.; every hour for 2 hours) elicits a dose-dependent reduction in infarct size (ED 50 =0.45 mg/kg/h) in open chest anesthetized rabbits . Zoniporide exhibits moderate plasma protein binding, has a t 1/2 of 1.5 hours in monkeys, and has one major active metabolite . Zoniporide hydrochloride hydrate treatment shows the AUC 0-∞ and t 1/2 are 0.07 μg h/mL and 0.5 hours, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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 ED 50 was 0.45 mg/kg/h. Animal Model: RatDosage: 1 mg/kg Administration: Intravenous injection(Pharmacokinetic Analysis) Result: The AUC 0-∞ and t 1/2 were 0.07 μg h/mL and 0.5 hours, respectively.Form:SolidIC50& Target:IC50: 14 nM (NHE-1). Specification: ≥99.0% Molecular Formula: C17H19ClN6O2 Molecular Weight: 374.82 PubChem CID: 22267662 Isomeric SMILES: C1CC1C2=C(C=NN2C3=CC=CC4=C3C=CC=N4)C(=O)N=C(N)N.O.Cl