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Zoniporide hydrochloride

Cat. No. M29629
Zoniporide hydrochloride Structure
Synonym:

CP-597396 hydrochloride

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Quality Control & Documentation
Biological Activity

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).

Chemical Information
Molecular Weight 356.81
Formula C17H17ClN6O
CAS Number 241800-97-5
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Gabriela Castañeda-Corral, et al. Brain Res. Blockade of peripheral and spinal Na+/H+ exchanger increases formalin-induced long-lasting mechanical allodynia and hyperalgesia in rats

[2] Ravi B Marala, et al. Eur J Pharmacol. Zoniporide: a potent and highly selective inhibitor of human Na(+)/H(+) exchanger-1

Related Na+/H+ Exchanger (NHE) Products
NHE3-IN-1

NHE3-IN-1 is an inhibitor of sodium/proton exchanger 3 (NHE-3).

NHE3-IN-2

NHE3-IN-2 is a Na+/H+ exchanger 3 (NHE3) inhibitor.

Eniporide

Eniporide (EMD 96785) is a Na(+)/H(+) exchange (NHE) inhibitor.

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).

BI-9627 hydrochloride 

BI-9627 hydrochloride is potent sodium-hydrogen exchanger isoform 1 (NHE1) inhibitor, with IC50s of 6 and 31 nM in intracellular pH recovery (pHi) and human platelet swelling assays, respectively. BI-9627 hydrochloride displays >30-fold selectivity against NHE2 and with no measurable inhibitory activity against the NHE3 isoform. BI-9627 hydrochloride shows low DDI (agent-agent interaction) potential, excellent pharmacokinetics in rat and dog, and remarkably potent activity in the isolated heart model of ischemia-reperfusion injury.

  Catalog
Abmole Inhibitor Catalog




Keywords: Zoniporide hydrochloride, CP-597396 hydrochloride supplier, Na+/H+ Exchanger (NHE) , inhibitors, activators


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