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E-4031 dihydrochloride (CAS 113559-13-0)

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Alternate Names:
4′-[[1-[2-(6-methyl-2-pyridyl)ethyl]-4-piperidinyl]carbonyl]-methanesulfonanilide
Application:
E-4031 dihydrochloride is a K+ channel blocker that spawned a class of antiarrhythmic molecules
CAS Number:
113559-13-0
Purity:
≥98%
Molecular Weight:
510.47
Molecular Formula:
C21H27N3O3S•2HCl•2H2O
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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E-4031 dihydrochloride is a compound of interest in cardiac electrophysiology research due to its influence on ion channels. This substance is well-known for its ability to selectively block the rapid component of the delayed rectifier potassium current (I_Kr), which is key to repolarization of the cardiac action potential. By inhibiting I_Kr, E-4031 dihydrochloride is utilized in studies exploring the mechanisms underlying cardiac arrhythmias and the prolongation of the QT interval on the electrocardiogram. It serves as a tool in the assessment of cardiotoxicity for new compounds, providing a reference for substance-induced QT interval prolongation. This compound is also instrumental in investigations of the genetic basis of certain arrhythmias, such as Long QT Syndrome, by simulating the effects of mutations that impair potassium channel function.


E-4031 dihydrochloride (CAS 113559-13-0) References

  1. The antiproliferative role of ERG K+ channels in rat osteoblastic cells.  |  Hernandez, L., et al. 2007. Cell Biochem Biophys. 47: 199-208. PMID: 17652772
  2. Acquisition of neuron-like electrophysiological properties in neuroblastoma cells by controlled expression of NDM29 ncRNA.  |  Gavazzo, P., et al. 2011. J Neurochem. 119: 989-1001. PMID: 21933186
  3. Functional characterization of ether-à-go-go-related gene potassium channels in midbrain dopamine neurons - implications for a role in depolarization block.  |  Ji, H., et al. 2012. Eur J Neurosci. 36: 2906-16. PMID: 22780096
  4. Characterization of loperamide-mediated block of hERG channels at physiological temperature and its proarrhythmia propensity.  |  Sheng, J., et al. 2017. J Pharmacol Toxicol Methods. 88: 109-122. PMID: 28830713
  5. Modulation of Ether-à-Go-Go Related Gene (ERG) Current Governs Intrinsic Persistent Activity in Rodent Neocortical Pyramidal Cells.  |  Cui, ED. and Strowbridge, BW. 2018. J Neurosci. 38: 423-440. PMID: 29175952
  6. Engineering of human cardiac muscle electromechanically matured to an adult-like phenotype.  |  Ronaldson-Bouchard, K., et al. 2019. Nat Protoc. 14: 2781-2817. PMID: 31492957
  7. Optimized Tuning of Auditory Inner Hair Cells to Encode Complex Sound through Synergistic Activity of Six Independent K+ Current Entities.  |  Dierich, M., et al. 2020. Cell Rep. 32: 107869. PMID: 32640234
  8. Mechanisms of QT prolongation by buprenorphine cannot be explained by direct hERG channel block.  |  Tran, PN., et al. 2020. PLoS One. 15: e0241362. PMID: 33157550
  9. Elevation of propofol sensitivity of cardiac IKs channel by KCNE1 polymorphism D85N.  |  Kojima, A., et al. 2021. Br J Pharmacol. 178: 2690-2708. PMID: 33763865
  10. hERG block potencies for 5 positive control drugs obtained per ICH E14/S7B Q&As best practices: Impact of recording temperature and drug loss.  |  Alvarez Baron, C., et al. 2022. J Pharmacol Toxicol Methods. 117: 107193. PMID: 35792285
  11. STRAIGHT-IN enables high-throughput targeting of large DNA payloads in human pluripotent stem cells.  |  Blanch-Asensio, A., et al. 2022. Cell Rep Methods. 2: 100300. PMID: 36313798
  12. Acute exposure to low-dose bisphenol A delays cardiac repolarization in female canine heart - Implication for proarrhythmic toxicity in large animals.  |  Ma, J., et al. 2023. Food Chem Toxicol. 172: 113589. PMID: 36584932
  13. Proarrhythmic toxicity of low dose bisphenol A and its analogs in human iPSC-derived cardiomyocytes and human cardiac organoids through delay of cardiac repolarization.  |  Ma, J., et al. 2023. Chemosphere. 328: 138562. PMID: 37004823

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

E-4031 dihydrochloride, 5 mg

sc-203034
5 mg
$286.00

Avrei necessità di trovare un inibitore che mi permetta di distinguere fra canali Kv10.1 e canali Kv11.1.

Asked by: Delfina
Thank you for your question. It would be helpful if you could call 800-457-3801, allowing for a more interactive discussion of this and other related questions.
Answered by: Tech Support Europe
Date published: 2022-08-03
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Rated 5 out of 5 by from BaiBai, X. et al. (PubMed 25330678) studied the effects of E-4031, a sodium calcium exchanger (NCX) agonist, on the isolated cardiac function and resting Ca2+ level in myocardial cells from rats with chronic heart failure. They found that E-4031 can improve the isolated heart function of rats with chronic heart failure, which may be associated with its enhancing the activity of NCX in the myocardial cell membrane and stabilizing intracellular Ca2+ level. -SCBT Publication Review
Date published: 2015-04-01
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E-4031 dihydrochloride | CAS 113559-13-0 is rated 5.0 out of 5 by 1.
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