Zoniporide hydrochloride
Modify Date: 2024-01-03 11:58:15
Zoniporide hydrochloride structure
|
Common Name | Zoniporide hydrochloride | ||
|---|---|---|---|---|
| CAS Number | 241800-97-5 | Molecular Weight | 393.270 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C17H18Cl2N6O | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of Zoniporide hydrochlorideZoniporide (CP-597396) hydrochloride is a potent and selective inhibitor of sodium-hydrogen exchanger type 1 (NHE-1). Zoniporide hydrochloride inhibits human NHE-1 (IC50=14 nM), and has >150-fold selectivity versus other NHE isoforms. Zoniporide hydrochloride potently inhibits ex vivo NHE-1-dependent swelling of human platelets (IC50=59 nM)[1][2]. |
| Name | Zoniporide dihydrochloride,[1-(Quinolin-5-yl)-5-cyclopropyl-1H-pyrazole-4-carbonyl]guanidinedihydrochloride |
|---|---|
| Synonym | More Synonyms |
| Description | Zoniporide (CP-597396) hydrochloride is a potent and selective inhibitor of sodium-hydrogen exchanger type 1 (NHE-1). Zoniporide hydrochloride inhibits human NHE-1 (IC50=14 nM), and has >150-fold selectivity versus other NHE isoforms. Zoniporide hydrochloride 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 (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 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 | C17H18Cl2N6O |
|---|---|
| Molecular Weight | 393.270 |
| Exact Mass | 392.091919 |
| PSA | 112.18000 |
| LogP | 4.71610 |
|
~%
Zoniporide hydr... CAS#:241800-97-5 |
| Literature: PFIZER PRODUCTS, INC. Patent: WO2005/79803 A1, 2005 ; Location in patent: Page/Page column 41 ; WO 2005/079803 A1 |
| Precursor 1 | |
|---|---|
| DownStream 0 | |
| N-Carbamimidoyl-5-cyclopropyl-1-(5-quinolinyl)-1H-pyrazole-4-carboxamide dihydrochloride |
| 1H-Pyrazole-4-carboxamide, N-(aminoiminomethyl)-5-cyclopropyl-1-(5-quinolinyl)-, hydrochloride (1:2) |
| zoniporide dihydrochloride |
| 5-Cyclopropyl-N-(diaminomethylene)-1-(quinolin-5-yl)-1H-pyrazole-4-carboxamide dihydrochloride |