E-4031 dihydrochloride

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本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

113559-13-0

包装与价格：

包装	价格(元)
5mg	电议
10mg	电议
50mg	电议

产品介绍

化学性质

Physical Appearance	A crystalline solid
Storage	Desiccate at RT
M.Wt	474.44
Cas No.	113559-13-0
Formula	C₂₁H₂₇N₃O₃S·2HCl
Solubility	Soluble in DMSO
Chemical Name	N-(4-(1-(2-(6-methylpyridin-2-yl)ethyl)piperidine-4-carbonyl)phenyl)methanesulfonamide dihydrochloride
Canonical SMILES	O=C(C(C=C1)=CC=C1NS(=O)(C)=O)C2CCN(CCC3=NC(C)=CC=C3)CC2.Cl.Cl
运输条件	蓝冰运输或根据您的需求运输。
一般建议	为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

E-4031 dihydrochloride is a methanesulfonanilide class Ⅲ antiarrhythmic agent, capable of prolonging cardiac action potential duration by blocking members of theether-a-go-go-related gene(ERG) K⁺channel family (IC50 = 29 nM). E-4031 dihydrochloride inhibits a variety of ERG isoforms, withK_Dvalues being 99, 116 and 193 nM for ERG1, ERG2 and ERG3, respectively. Voltage-gated potassium ERG channels regulate the inwardly rectifying K⁺current that repolarizes myocardial cells, gut smooth muscle cells, as well as interstitial cells of Cajal. E-4031 dihydrochloride, as a human ERG (hERG; also known as Kv11.1) K⁺channel blocker, has been used to pharmacologically rescue misprocessed hERG mutations in the long QT syndrome type 2.

References:

1. Du LP, Tsai KC, Li MY, et al. The pharmacophore hypotheses of I(Kr) potassium channel blockers: novel class III antiarrhythmic agents. Bioorganic & Medicinal Chemistry Letters, 2004, 14(18): 4771-4777.

2. Shi W, Wymore RS, Wang HS, et al. Identification of two nervous system-specific members of the erg potassium channel gene family. Journal of Neuroscience, 1997, 17(24): 9423-9432.

3. White EJ, Park SJ, Foster JA, et al. Ether-a-go-go-related gene 3 is the main candidate for the E-4031-sensitive potassium current in the pacemaker interstitial cells of Cajal. American Journal of Physiology-Gastrointestinal and Liver Physiology, 2008, 295(4): G691-699.

4. Ficker E, Obejero-Paz CA, Zhao S, et al. The binding site for channel blockers that rescue misprocessed human long QT syndrome type 2 ether-a-gogo-related gene (HERG) mutations. Journal of Biological Chemistry, 2002, 277(7): 4989-4998.

5. Fujiki A. Electrophysiological effects of E-4031, a novel class Ⅲ antiarrhythmic agent. Cardiovascular Drun Reviews, 1994, 12(2): 165-172.

试验操作

Cell experiment:[3]
Cell lines	Mouse small intestine musculature
Reaction Conditions	1 or 2 μM E-4031
Applications	E-4031 induced a significant depolarization of the musculature at 1 μM, probably due to block of ERG channels in smooth muscle cells as well as interstitial cells of Cajal. Further depolarization was seen with 2 μM E-4031.
Animal experiment:[5]
Animal models	Conscious dogs 3 ~ 5 days after anterior myocardial infarction
Dosage form	Loading dose 100 μg/kg E-4031 Followed by infusion of 10 μg/kg/min E-4031
Applications	E-4031 suppressed the induction of ventricular tachycardia by programmed electrical stimulation. E-4031 protected dogs from the development of ventricular fibrillation within the first hour after the onset of myocardial ischemia in a region remote from the infarcted area.
Note	The technical data provided above is for reference only.
	References: 1. Du LP, Tsai KC, Li MY, et al. The pharmacophore hypotheses of I(Kr) potassium channel blockers: novel class III antiarrhythmic agents. Bioorganic & Medicinal Chemistry Letters, 2004, 14(18): 4771-4777. 2. Shi W, Wymore RS, Wang HS, et al. Identification of two nervous system-specific members of the erg potassium channel gene family. Journal of Neuroscience, 1997, 17(24): 9423-9432. 3. White EJ, Park SJ, Foster JA, et al. Ether-a-go-go-related gene 3 is the main candidate for the E-4031-sensitive potassium current in the pacemaker interstitial cells of Cajal. American Journal of Physiology-Gastrointestinal and Liver Physiology, 2008, 295(4): G691-699. 4. Ficker E, Obejero-Paz CA, Zhao S, et al. The binding site for channel blockers that rescue misprocessed human long QT syndrome type 2 ether-a-gogo-related gene (HERG) mutations. Journal of Biological Chemistry, 2002, 277(7): 4989-4998. 5. Fujiki A. Electrophysiological effects of E-4031, a novel class Ⅲ antiarrhythmic agent. Cardiovascular Drun Reviews, 1994, 12(2): 165-172.