Overview
Cat #:
E-500
Lyophilized Powder yes
Source Synthetic
MW: 510.5
Purity: >98%
Effective concentration 100 nM - 1 μM.
Structure
Chemical name (1-[2-(6-Methyl-2-pyridyl)ethyl]-4-(4-methylsulfonyl-aminobenzoyl)piperidine).
Molecular formula C21H27N3O3S•2HCl•2H2O.
CAS No.: 113559-13-0
Activity E-4031 is a methsnesulfonanilide class III antiarrhythmic agent. It specifically blocks hERG (KV11.1) voltage-gated K+ channel current in heterologous systems1,2, cardiac cells3 and cardiac preparations4.
References-Activity
- Spector, P.S. et al. (1996) Circ. Res. 78, 499.
- Zhou, Z. et al. (1998) Biophys. J. 74, 230.
- Sanguinetti, M.C. and Jurkiewicz, N.K. (1990) J. Gen. Physiol. 96, 195.
- Wettwer, E. et al. (1991) J. Cardiovasc. Pharmacol. 17, 480.
Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
Solubility Any aqueous buffer. Centrifuge all product preparations before use (10000 x g 5 min).
Storage of solutions Up to one week at 4°C or six months at -20°C.
Our bioassay
Alomone Labs E-4031 inhibits HERG K+ currents heterologously expressed in HEK-293 cells.Top: Traces of KV11.1 currents elicited every 5 seconds from a holding potential of -100 mV, by a compound test pulse (250 ms at +20 mV followed by 250 ms at -40 mV), before (blue) and during (green) application of 1 μM E-4031 (#E-500). Bottom: Dose-response relationship describing the inhibition of KV11.1 currents by increasing concentrations of E-4031. IC50 was at about 500 nM. Data and SD values for n = 4-9 are given.
References - Scientific background
- Spector, P.S. et al. (1996) Circ Res. 78, 499.
- Zhou, Z. et al. (1998) Biophys. J. 74, 230.
- Sanguinetti, M.C. and Jurkiewicz, N.K. (1990) J. Gen Physiol. 96, 195.
- Wettwer, E. et al. (1991) J. Cardiovasc. Pharmacol. 17, 480.
- Anderson, C.L. et al. (2006) Circulation 113, 365.
- Cherubini, A. et al. (2005) Mol. Biol. Cell 16, 2972.
- Kim, I. et al. (2005) J. Appl. Physiol. 98, 1469.
- Liu, J.H. et al. (2003) Development 130, 3437.
Scientific background E-4031 is a methanesulfonanilide class III antiarrhythmic agent known to inhibit KV11.1 (hERG) channels. Sub-micromolar concentration of E-4031, selectively blocks Kv11.1 channels, either in heterologous systems,1,2 cardiac cells3 and cardiac preparations.4 E-4031 was shown to rescue the functional expression of mutated (LQ2) KV11.1 channels in HEK cells.5 E-4031 (40 µM) treatment also prevented FAK phosphorylation and Rac1 activity (only in HEK cells expressing the KV11.1 subunit).6 In rat carotid chemoreceptor cells, 1 µM E-4031 inhibited the KV current, to a larger extent in postnatal cells, establishing the developmental disappearance of KV11.1 channels and their contribution to the response to hypoxia.7 E-4031 (1 µM) accelerated myoblast fusion, probably by blocking KV11.1 channels that leads to depolarization.8
Target KV11.1 K+ channels
Lyophilized Powder
E-4031 (#E-500) is a highly pure, synthetic, and biologically active compound.
Image & Title 
Alomone Labs E-4031 blocks hERG channels in HEK 293 transfected cells.Current vs voltage (I-V) curve before and after application of 1 µM E-4031 (#E-500) to cells.Adapted from Schlichter, L.C. et al. (2014) PLoS ONE 9, e90024. with permission of PLoS.
Alomone Labs E-4031 blocks hERG channels in HEK 293 transfected cells.Current vs voltage (I-V) curve before and after application of 1 µM E-4031 (#E-500) to cells.Adapted from Schlichter, L.C. et al. (2014) PLoS ONE 9, e90024. with permission of PLoS.
For research purposes only, not for human use
Last Update: 31/10/2023
Applications
Citations
Citations
Powered by BiozProduct citations
- Altomare, C. et al. (2016) Europace 18, iv67.
- Schlichter, L.C. et al. (2014) PLoS ONE 9, e90024.
- Wondergem, R. et al. (2012) Am. J. Physiol. 303, C825.
