ChemicalBook CAS DataBase List 863406-85-3

863406-85-3

Name	Zoniporide hydrochloride hydrate
CAS	863406-85-3
Molecular Formula	C17H19ClN6O2
Molecular Weight	374.83
MOL File	863406-85-3.mol

Chemical Properties

storage temp.	Store at -20°C
solubility	Soluble in DMSO
form	Solid
color	White to off-white

Hazard Information

Uses

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].

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 t_1/2 of 1.5 hours in monkeys, and has one major active metabolite^[1].
Zoniporide hydrochloride hydrate treatment shows the AUC_0-∞ and t_1/2 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 AUC_0-∞ and t_1/2 were 0.07 μg h/mL and 0.5 hours, respectively.

storage

Store at -20°C

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. DOI:10.1111/j.1527-3466.2003.tb00103.x
[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. DOI:10.1016/s0960-894x(01)00059-2

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