For research use only. Not for therapeutic Use.
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].
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].
| Catalog Number | I017493 |
| CAS Number | 863406-85-3 |
| Synonyms | 5-cyclopropyl-N-(diaminomethylidene)-1-quinolin-5-ylpyrazole-4-carboxamide;hydrate;hydrochloride |
| Molecular Formula | C17H19ClN6O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C17H16N6O.ClH.H2O/c18-17(19)22-16(24)12-9-21-23(15(12)10-6-7-10)14-5-1-4-13-11(14)3-2-8-20-13;;/h1-5,8-10H,6-7H2,(H4,18,19,22,24);1H;1H2 |
| InChIKey | UCIJUEGJEFJRMP-UHFFFAOYSA-N |
| SMILES | C1CC1C2=C(C=NN2C3=CC=CC4=C3C=CC=N4)C(=O)N=C(N)N.O.Cl |
| Reference | [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. |
