E-4031 | Alomone Labs E-500 product information

product summary

company name :

Alomone Labs

product type :

chemical

product name :

E-4031

catalog :

E-500

more info or order :

Alomone Labs product webpage

citations: 11

Reference
Hall A, Anderson C, Smith J, Mirshahi T, Elayi C, January C, et al. Visualizing Mutation-Specific Differences in the Trafficking-Deficient Phenotype of Kv11.1 Proteins Linked to Long QT Syndrome Type 2. Front Physiol. 2018;9:584 pubmed publisher
Altomare C, Pianezzi E, Cervio E, Bolis S, Biemmi V, Benzoni P, et al. Human-induced pluripotent stem cell-derived cardiomyocytes from cardiac progenitor cells: effects of selective ion channel blockade. Europace. 2016;18:iv67-iv76 pubmed publisher
Kuusela J, Kujala V, Kiviaho A, Ojala M, Swan H, Kontula K, et al. Effects of cardioactive drugs on human induced pluripotent stem cell derived long QT syndrome cardiomyocytes. Springerplus. 2016;5:234 pubmed publisher
Shinnawi R, Huber I, Maizels L, Shaheen N, Gepstein A, Arbel G, et al. Monitoring Human-Induced Pluripotent Stem Cell-Derived Cardiomyocytes with Genetically Encoded Calcium and Voltage Fluorescent Reporters. Stem Cell Reports. 2015;5:582-96 pubmed publisher
Lin E, Moungey B, Lim E, Concannon S, Anderson C, Kyle J, et al. Mouse ERG K(+) channel clones reveal differences in protein trafficking and function. J Am Heart Assoc. 2014;3:e001491 pubmed publisher
Anderson C, Kuzmicki C, Childs R, Hintz C, Delisle B, January C. Large-scale mutational analysis of Kv11.1 reveals molecular insights into type 2 long QT syndrome. Nat Commun. 2014;5:5535 pubmed publisher
Ferro F, Ouillé A, Tran T, Fontanaud P, Bois P, Babuty D, et al. Long-chain acylcarnitines regulate the hERG channel. PLoS ONE. 2012;7:e41686 pubmed publisher
Lahti A, Kujala V, Chapman H, Koivisto A, Pekkanen Mattila M, Kerkela E, et al. Model for long QT syndrome type 2 using human iPS cells demonstrates arrhythmogenic characteristics in cell culture. Dis Model Mech. 2012;5:220-30 pubmed publisher
Schaaf S, Shibamiya A, Mewe M, Eder A, Stöhr A, Hirt M, et al. Human engineered heart tissue as a versatile tool in basic research and preclinical toxicology. PLoS ONE. 2011;6:e26397 pubmed publisher
Vornanen M, Hälinen M, Haverinen J. Sinoatrial tissue of crucian carp heart has only negative contractile responses to autonomic agonists. BMC Physiol. 2010;10:10 pubmed publisher
Sauviat M, Colas A, Pages N. Does lindane (gamma-hexachlorocyclohexane) increase the rapid delayed rectifier outward K+ current (IKr) in frog atrial myocytes?. BMC Pharmacol. 2002;2:15 pubmed

image

image 1 :

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 ?ME-4031(#E-500). Bottom: Dose-response relationship describing the inhibition of KV11.1 currents by increasing concentrations of E-4031. IC50was at about 500 nM. Data and SD values forn= 4-9 are given.

image 2 :

Alomone Labs49-Anhydrotetrodotoxin selectively blocks NaV1.6 channels expressed inXenopusoocytes. - A. Time course of49-Anhydrotetrodotoxin(#T-560) inhibition of NaV1.6 maximum current amplitude. Membrane potential was held at -100 mV and currents were elicited by a 100 ms voltage step to 0 mV every 10 sec. 49-Anhydrotetrodotoxin applied at 10 nM and 50 nM as indicated (bars) reversibly inhibits NaV1.6 currents in a concentration dependent manner. B. Superimposed traces of NaV1.6 current upon application of control and of 10 nM and 50 nM 49-Anhydrotetrodotoxin (as indicated) taken from the recording shown in A.

product information

CAT :

E-500

SKU :

E-500_0.5 mg

Product Name :

E-4031

Group Type :

Non Antibodies

Product Type :

S. Molecules

Storage After Reconstitution :

The reconstituted solution can be stored at 4°C for up to 1 week. For longer periods (up to 6 months), small aliquots should be stored at -20°C. We do not recommend storing the product in working solutions for longer than a few days. Avoid multiple freeze-thaw cycles.

Storage before Reconstitution :

The product is shipped as a lyophilized powder at room temperature. Upon receipt, store the product at -20°C. Protect from moisture.

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

Product Page - 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

Supplier :

Alomone Labs

Target :

KV11.1 K+ channels

Long Description :

E-4031 (#E-500) is a highly pure, synthetic, and biologically active compound.

Short Description :

A Blocker of KV11.1 (hERG) K+ Channels

MW :

510.5

Source :

Synthetic

Molecular formula :

C21H27N3O3S•2HCl•2H2O.

Effective Concentration :

100 nM - 1 μM.

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.

Reconstitution and Solubility :

Centrifuge the vial before adding solvent (10,000 x g for 5 minutes) to spin down all the powder to the bottom of the vial. The lyophilized product may be difficult to visualize. Add solvent directly to the centrifuged vial. Tap the vial to aid in dissolving the lyophilized product. Tilt and gently roll the liquid over the walls of the vial. Avoid vigorous vortexing. Light vortexing for up to 3 seconds is acceptable if needed. For long-term storage in solution, we recommend preparing a stock solution by dissolving the product in sterile water at a concentration of at least 0.1 mg/mL. Divide the stock solution into small aliquots and store at -20°C. Before use, thaw the relevant vial(s) and dilute to the desired working concentration in your working buffer. It is recommended to prepare fresh solutions in working buffers just before use. For long-term storage of diluted solutions, we recommend adding 0.1% BSA. Repeat freeze-thawing may result in loss of activity.

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.

Lead Time :

1-2 Business Days

Country of origin :

Israel/IL

Applications key :

Application key: FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay.

Purity :

>98%

CAS No :

113559-13-0

Form :

Lyophilized powder.

Comment :

Contact Alomone Labs for technical support and product customization

UNSPSC :

41116134

Bioassay Tested :

Yes

Cited Application :

Electrophysiology

Chemical Name :

(1-[2-(6-Methyl-2-pyridyl)ethyl]-4-(4-methylsulfonyl-aminobenzoyl)piperidine).

more info or order :

Alomone Labs product webpage