Cardiotoxic Compounds

In drug development, ensuring the safety of new medications is paramount, particularly concerning cardiotoxicity. The human ether-a-go-go-related gene (hERG) encodes a potassium channel crucial for cardiac repolarization, influencing the heart's electrical activity and action potential regulation. Compounds that block the hERG potassium channel can lead to life-threatening arrhythmias, notably Torsades de Pointes, due to disruptions in cardiac rhythm. This underscores the importance of assessing cardiotoxicity. Developing safe medications requires a comprehensive understanding of the pharmacokinetic profile, particularly regarding cardiotoxic effects. The proposed library can facilitate hERG potassium channel screening, aiding in the assessment of cardiotoxic safety for compounds of interest.

Library of Сardiotoxic Сompounds contains 327 intense inhibitors/blockers of hERG potassium channel with biological activity data.

Related terms: hERG, ion channel, potassium channel, toxicology, Kv11.1

A) Cryo-EM structure of K⁺-bound hERG channel.

B) Topology of Kv11.1 or hERG channel.

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Preplated options

Dry powder/solution (DMSO)Dry powder

Number of compounds327

Comment

Dry powder/solution (DMSO)DMSO

Number of compounds271

Comment

Highlights

EBC-26698CAS: 66778-36-7

Encainide is a voltage-gated sodium channel blocker.

EBC-11108CAS: 1744-22-5

Riluzole is a glutamate antagonist used as an anticonvulsant.

EBC-47130CAS: 1842349-15-8

This compound inhibits indoleamine 2,3-dioxygenase.

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All our products are for research purpose only. Any personal or non-scientific use is strictly prohibited.

Note

All the compounds with solubility below 10 mM are shipped as 2 mM solutions.

Product Features

Library of Cardiotoxic Compounds is a set of 327 bioactive molecules for HTS/HCS programs.
Library of Cardiotoxic Compounds covers novel promising preclinical lead compounds, clinical candidates and approved drugs.
Comprehensive documentation with structures, trivial names, synonyms, activity coefficient values, types of action on target and references to original literature.
Calculated structural diversity of the collection: 0.85.
NMR and LCMS validated purity.
All the compounds are available in stock for hit follow-up.
The library is continuously updated.

Product Details

Format: 10 - 100 µL of 10 mM DMSO stock solutions; dry powders (1 mg);
Container: 384-well microplates;
Storage: - 18 °C;
Shipping: Dry ice.

Utility

High throughput screening (HTS);
High content screening (HCS);
Cherry picking.