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Eniporide

Cat. No. M42811
Eniporide Structure
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Biological Activity

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

Chemical Information
Molecular Weight 320.37
Formula C14H16N4O3S
CAS Number 176644-21-6
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
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] Venkatesh Atul Bhattaram et al. J Clin Pharmacol. Population pharmacokinetics of eniporide and its metabolite in healthy subjects and patients with acute myocardial infarction

[2] Oliver Klass et al. Ann Thorac Surg. Effect of the Na+/H+ exchange inhibitor eniporide on cardiac performance and myocardial high energy phosphates in pigs subjected to cardioplegic arrest

[3] Metin Avkiran et al. J Am Coll Cardiol. Na(+)/H(+) exchange inhibitors for cardioprotective therapy: progress, problems and prospects

[4] U Zeymer et al. J Am Coll Cardiol. The Na(+)/H(+) exchange inhibitor eniporide as an adjunct to early reperfusion therapy for acute myocardial infarction. Results of the evaluation of the safety and cardioprotective effects of eniporide in acute myocardial infarction (ESCAMI) trial

[5] A Kovar et al. J Clin Pharmacol. Pharmacokinetic/pharmacodynamic evaluation of the NHE inhibitor eniporide

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.
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).
Zoniporide hydrochloride

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).
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.
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Keywords: Eniporide supplier, Na+/H+ Exchanger (NHE) , inhibitors, activators

 
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