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Tocris/E-4031 dihydrochloride/1808/50/50 mg

价格: ¥9180.00 市场价: 15300.00

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货号: 1808/50

品牌: Tocris

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Description: K_V11.1 (hERG) channel blocker; inhibits rapid delayed rectifier K⁺ current (I_Kr)

Chemical Name: N-[4-[[1-[2-(6-Methyl-2-pyridinyl)ethyl]-4-piperidinyl]carbonyl]phenyl]methanesulfonamide dihydrochloride

Purity: ≥98% (HPLC)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

Selective blocker of K_V11.1 (hERG) channels; inhibits the rapid delayed-rectifier K⁺ current (I_Kr). Reversibly prolongs action potential duration in guinea pig papillary muscle and isolated ventricular myocytes, without affecting Na⁺ or Ca²⁺ inward currents. Class III antiarrhythmic agent.

Compound Libraries

E-4031 dihydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt	474.44
Formula	C₂₁H₂₇N₃O₃S.2HCl
Storage	Desiccate at RT
Purity	≥98% (HPLC)
CAS Number	113559-13-0
PubChem ID	3087190
InChI Key	ZQBNWMFBOSOOLX-UHFFFAOYSA-N
Smiles	Cl.Cl.CC1=CC=CC(CCN2CCC(CC2)C(=O)C2=CC=C(NS(C)(=O)=O)C=C2)=N1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	23.72	50
	water	47.44	100

Preparing Stock Solutions

The following data is based on the product molecular weight 474.44. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.11 mL	10.54 mL	21.08 mL
5 mM	0.42 mL	2.11 mL	4.22 mL
10 mM	0.21 mL	1.05 mL	2.11 mL
50 mM	0.04 mL	0.21 mL	0.42 mL

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

Ficker et al (2002) The binding site for channel blockers that rescue misprocessed human long QT syndrome type 2 ether-a-gogo-related gene (HERG) mutations. J.Biol.Chem. 277 4989 PMID: 11741928

Verheijck et al (1995) Effects of the delayed rectifier current blockade by E-4031 on impulse generation in single sinoatrial nodal myocytes of the rabbit. Circ.Res. 76 607 PMID: 7895335

Wettwer et al (1991) Effects of the new class III antiarrhythmic drug E-4031 on myocardial contractility and electrophysiological parameters. J.Cardiovasc.Pharmacol. 17 480 PMID: 1711611

Keywords: E-4031 dihydrochloride, supplier, HERG, KV11.1, channel, blockers, inhibits, inhibitors, rapid, delayed, rectifier, K+, current, IKr, Potassium, KV, Channels, Human, Ether-A-Go-Go, Gene, voltage-gated, voltage-dependent, Voltage-Gated, Potassium, Channels, Voltage-Gated, Potassium, Channels, Tocris Bioscience

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