Potassium Channel Blockers
     
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Potassium Channel Blockers

Kv1.5 Potassium Channel BlockerAtrial fibrillation is the most common sustained cardiac rhythm disorder, and confers a substantial mortality and morbidity from stroke, thromboembolism, heart failure, and impaired quality of life. With the increasingly elderly population in the developed world, the prevalence of atrial fibrillation is increasing, resulting in a major public-health problem.

The ultra-rapid delayed rectifier potassium current (IKur), encoded by Kv1.5 gene, is a selective target for the treatment of atrial fibrillation.
 
The Kv1.5 Potassium Channel Targeted Library (876 compounds in total) has been designed as a special screening library containing compounds with predicted Kv1.5 blocking activity. A four-center pharmacophore model developed by Yang et al which includes one aromatic ring, two hydrophobic points, and a hydrogen-bond acceptor has been used for the library design. The model was derived from forty Kv1.5 blocker compounds with distinct chemical structure types. We opted this pharmacophore model for virtual screening of OTAVAchemicals Drug-like Green Collection.
 
This library comprises drug-like compounds only and provides an excellent basis for ion channel-related research and drug discovery projects.

 

All compounds are in stock, cherry-picking is available.

 

The library (DB, SD, XLS, PDF format) as well as the price-list is available on request. Feel free to contact us or use on-line form below to send an inquiry if you are interested to obtain this library or if you need more information.

 


 

References:

  • G. Y. Lip, H. F. Tse. Management of atrial fibrillation. Lancet 2007, 370(9587), 604 – 618.
  • R. L. Page, D. M. Roden. Drug therapy for atrial fibrillation: where do we go from here? Nat. Rev. Drug Discov. 2005, 4(11), 899 – 910.
  • Ravens U, Odening KE. Atrial fibrillation: Therapeutic potential of atrial K+ channel blockers. Pharmacol Ther. 2017 Aug;176:13-21.
  • Zhao Z, Ruan S, Ma X et al. Challenges Faced with Small Molecular Modulators of Potassium Current Channel Isoform Kv1.5. Biomolecules. 2019 Dec 19;10(1):10.
  • Yang Q, Du L, Tsai K-C et al. Pharmacophore Mapping for Kv1.5 Potassium Channel Blockers. QSAR Comb Sci 2009, 28, 59–71.
 

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