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 Vivo Zoniporide 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:Solid IC50& Target:IC50: 14 nM (NHE-1)
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Zoniporide hydrochloride hydrate
CAS number：863406-85-3 molecular formula：C17H19ClN6O2
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| Chinese alias | 佐尼泊利德盐酸盐水合物 | ||
| English alias | 5-cyclopropyl-N-(diaminomethylidene)-1-quinolin-5-ylpyrazole-4-carboxamide;hydrate;hydrochloride | 70297XU9ZO | MS-26069 | SCHEMBL6263279 | N-(Aminoiminomethyl)-5-cyclopropyl-1-(5-quinolinyl)-1H-pyrazole-4-carboxamide hydrochloride hydrate | HY-105064D | | ||
| CAS number | 863406-85-3 | molecular formula | C17H19ClN6O2 |
| molecular weight | 374.82 g/mol | Exact mass | ≥99% |
| PSA | 113.000 Ų | logp | - |
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