863406-85-3
863406-85-3 structure
- Name: Zoniporide hydrochloride hydrate
- Chemical Name: 5-cyclopropyl-N-(diaminomethylidene)-1-quinolin-5-ylpyrazole-4-carboxamide,hydrate,hydrochloride
- CAS Number: 863406-85-3
- Molecular Formula: C17H19ClN6O2
- Molecular Weight: 374.82500
- Catalog: Signaling Pathways Membrane Transporter/Ion Channel Sodium Channel
- Create Date: 2017-09-17 03:03:09
- Modify Date: 2024-01-12 06:51:55
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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].
| Name | 5-cyclopropyl-N-(diaminomethylidene)-1-quinolin-5-ylpyrazole-4-carboxamide,hydrate,hydrochloride |
|---|---|
| Synonyms |
Zoniporide hydrochloride monohydrate
Zoniporide monohydrochloride monohydrate |
| Description | 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]. |
|---|---|
| Related Catalog | |
| Target |
IC50: 14 nM (NHE-1)[1] |
| 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. |
| References |
| Molecular Formula | C17H19ClN6O2 |
|---|---|
| Molecular Weight | 374.82500 |
| Exact Mass | 374.12600 |
| PSA | 122.40000 |
| LogP | 4.03370 |
| Hazard Codes | Xi |
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