Key result
Compound 12 was discovered as a novel potent and selective reverse NCX inhibitor with an IC50 value of 0.085 μM, demonstrating approximately 3-times greater potency than SEA0400.
Absolute Event Rate: 0.085% vs 0.29%
The discovery of compound 12 provides a potent and selective reverse NCX inhibitor that may serve as a lead compound for developing treatments for heart failure and myocardial ischemia-reperfusion injury.
May advance NCX inhibitor development for HF and I/R injury; leaves open clinical translation.
In the setting of heart failure and myocardial ischemia-reperfusion, the sodium-calcium exchanger (NCX) can lead to calcium overload, which is responsible for contractile dysfunction and arrhythmia. NCX is an attractive target for treatment in heart failure and myocardial ischemia-reperfusion. We have designed and synthesized a series of benzyloxyphenyl derivatives based on compound 3. These derivatives have been evaluated for their inhibitory activity against both the reverse and forward modes of NCX. We have discovered a novel potent and selective reverse NCX inhibitor (12) with an IC50 value of 0.085 microM against reverse NCX.
No takes yet. Share an insight, caveat, or question.
Kuramochi et al. (2005) studied Myocardial ischemia-reperfusion injury. Compound 12 (N-(3-{4-[(3-Fluorobenzyl)oxy]phenoxy}propyl)-2-pyridin-4-ylacetamide) vs. SEA0400 was evaluated on Inhibitory activity against reverse NCX (IC50 in μM). Compound 12 was discovered as a novel potent and selective reverse NCX inhibitor with an IC50 value of 0.085 μM, demonstrating approximately 3-times greater potency than SEA0400.
Synapse has enriched 5 closely related papers on similar clinical questions. Consider them for comparative context: