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Merck

SML0076

Zoniporide hydrochloride hydrate

≥98% (HPLC), sodium-hydrogen exchanger isoform 1 (NHE-1) inhibitor, powder

Synonym(s):

N-(Aminoiminomethyl)-5-cyclopropyl-1-(5-quinolinyl)-1H-pyrazole-4-carboxamide hydrochloride hydrate

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About This Item

Empirical Formula (Hill Notation):
C17H16N6O · xHCl · yH2O
CAS Number:
Molecular Weight:
320.35 (anhydrous free base basis)
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
Storage condition:
desiccated
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Product Name

Zoniporide hydrochloride hydrate, ≥98% (HPLC)

Quality Level

assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

white to tan

solubility

H2O: 2 mg/mL, clear (warmed)

storage temp.

2-8°C

SMILES string

O.Cl.NC(=N)NC(=O)c1cnn(-c2cccc3ncccc23)c1C4CC4

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

InChI key

UCIJUEGJEFJRMP-UHFFFAOYSA-N

Application

Zoniporide hydrochloride hydrate may be used in Na+/H+-mediated cell signaling studies.
Zoniporide hydrochloride hydrate has been used for the inhibition of sodium-hydrogen exchanger isoform 1 (NHE-1) in rat models. It has also been used in cytotoxicity assay and to study its effect on lymphocytic choriomeningitis virus multiplication.

Biochem/physiol Actions

Potent and selective inhibitor of Na+/H+ exchanger isoform 1 (NHE-1)
Zoniporide is a potent and selective inhibitor of Na+/H+ exchanger isoform 1 (NHE-1). IC50 = 59 nM at NHE-1, vs. 12,000 nM at NHE-2; Zoniporide inhibits NHE-1-dependent Na+ update with IC50 of 14 nM.
Zoniporide, a selective inhibitor of sodium-hydrogen exchanger isoform 1 (NHE-1) has cardioprotective effects against myocardial injuries and ischemic insults. It inhibits the swelling human platelets and attenuates cardiac contractile dysfunction in rats. Zoniporide might have neurotoxic effects as it causes peripheral sensory axonopathy.


Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



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W Ross Tracey et al.
Cardiovascular drug reviews, 21(1), 17-32 (2003-02-22)
The sodium-hydrogen exchanger isoform-1 (NHE-1) plays an important role in the myocardial response to ischemia-reperfusion; inhibition of this exchanger protects against ischemic injury, including reduction in infarct size. Herein we describe a novel, potent, and highly selective NHE-1 inhibitor, zoniporide
Adverse postresuscitation myocardial effects elicited by buffer-induced alkalemia ameliorated by NHE-1 inhibition in a rat model of ventricular fibrillation
Lamoureux L, et al.
Journal of Applied Physiology, 121(5), 1160-1168 (2016)
D R Knight et al.
The Journal of pharmacology and experimental therapeutics, 297(1), 254-259 (2001-03-22)
The cardioprotective efficacy of zoniporide (CP-597,396), a novel, potent, and selective inhibitor of the sodium-hydrogen exchanger isoform 1 (NHE-1), was evaluated both in vitro and in vivo using rabbit models of myocardial ischemia-reperfusion injury. In these models, myocardial injury was



Global Trade Item Number

SKUGTIN
SML0076-10MG04061832575957
SML0076-50MG04061832575964