E-4031
- 貨號 Cat. No.
- E-500
- 規格 Size
- 0.1 mg 5x0.1mg 0.5mg 1mg
Description
E-4031
A Blocker of Kv11.1 (hERG) K+ Channels
| Product#: | E-500 |
| Sizes: |
| 0.1 mg |
| 5 x 0.1 mg |
| 0.5 mg |
| 1 mg |
| M.W.: | 510.48 |
| Purity: | >98% |
| Bioassay: |
| Inhibition of KV11.1 (HERG) channels expressed in HEK-293 cells by E-4031. |
 |
E-4031 fully inhibits Kv11.1 current expressed in HEK-293 cells (above). 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 (black) and during (pink) application of 1 mM E-4031. Bottom: Dose response relationship describing the inhibition of Kv11.1 currents expressed in HEK-293 by increasing concentrations of E-4031. IC50 was at about 500 nM. Data and SD values for n=4-9 is given.
|
| References: |
1. | Spector, P.S. et al. (1996) Circ Res. 78, 499. |
2. | Zhou, Z. et al. (1998) Biophys.J. 74, 230. |
3. | Sanguinetti, M.C. and Jurkiewicz, N.K. (1990) J. Gen Physiol. 96, 195. |
4. | Wettwer, E. et al. (1991) J. Cardiovasc. Pharmacol. 17, 480. |
5. | Anderson, C.L. et al. (2006) Circulation 113, 365. |
6. | Cherubini, A. et al. (2005) Mol. Biol. Cell 16, 2972. |
7. | Kim, I. et al. (2005) J. Appl. Physiol. 98, 1469. |
8. | Liu, J.H. et al. (2003) Development 130, 3437. |
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 mM) treatment also prevented FAK phosphorylation and Rac1 activity (only in HEK cells expressing the KV11.1 subunit).6 In rat carotid chemoreceptor cells, 1 mM 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 mM) accelerated myoblast fusion, probably by blocking KV11.1 channels that leads to depolarization.8