Zoniporide hydrochloride hydrate

Modify Date: 2024-01-12 06:51:55

Zoniporide hydrochloride hydrate Structure
Zoniporide hydrochloride hydrate structure
Common Name Zoniporide hydrochloride hydrate
CAS Number 863406-85-3 Molecular Weight 374.82500
Density N/A Boiling Point N/A
Molecular Formula C17H19ClN6O2 Melting Point N/A
MSDS USA Flash Point N/A

 Use of Zoniporide hydrochloride hydrate


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].

 Names

Name 5-cyclopropyl-N-(diaminomethylidene)-1-quinolin-5-ylpyrazole-4-carboxamide,hydrate,hydrochloride
Synonym More Synonyms

 Zoniporide hydrochloride hydrate Biological Activity

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

[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.

[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.

 Chemical & Physical Properties

Molecular Formula C17H19ClN6O2
Molecular Weight 374.82500
Exact Mass 374.12600
PSA 122.40000
LogP 4.03370

 Safety Information

Hazard Codes Xi

 Synonyms

Zoniporide hydrochloride monohydrate
Zoniporide monohydrochloride monohydrate
The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.
Top Suppliers:I want be here



Get all suppliers and price by the below link:

Zoniporide hydrochloride hydrate suppliers


Price: ¥1600/1 mg

Reference only. check more Zoniporide hydrochloride hydrate price