Size | Price | Stock | Qty |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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Purity: ≥98%
E-4031 diHCl (E4031 dihydrochloride) is a novel, potent and selective blocker of hERG K+ channels, which is also termed as a class III antiarrhythmic agent. It selectively blocks hERG potassium (K+) channels. E4031 inhibits the rapid delayed-rectifier K+ current (IKr) and reversibly prolongs action potential duration in guinea pig papillary muscle and isolated ventricular myocytes, without affecting Na+ or Ca2+ inward currents.
ln Vitro |
Maximum diastolic potential (MDP) of single SAN cells in New Zealand white rabbits is significantly de-longitudated by E-4031 (0.1 ~ 10 μM), resulting in the MDP de-longest action scaffold from -58.8±0.9 mV at 1 μM Extended to -24.5±1.8 mV and from -58.2±2.1 to -19.6±1.8 mV at 10 μM[2]. In a dose-dependent manner, E-4031 (0.1 ~ 10 μM) inhibits the depolarization process. In single SAN cells of New Zealand white rabbits, the partial external current and subsequent tail current (ITD) during the complex partial process resulted in an 88% [sup] reduction in ITD [2].
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References |
[1]. Daisuke Izumi, et al. Effects of bepridil versus E-4031 on transmural ventricular repolarization and inducibility of ventricular tachyarrhythmias in the dog. Pacing Clin Electrophysiol. 2010 Aug;33(8):950-9.
[2]. E E Verheijck, et al. Effects of delayed rectifier current blockade by E-4031 on impulse generation in single sinoatrial nodal myocytes of the rabbit. Circ Res. 1995 Apr;76(4):607-15. |
Molecular Formula |
C21H29CL2N3O3S
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Molecular Weight |
474.4443
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Exact Mass |
401.18
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Elemental Analysis |
C, 53.16; H, 6.16; Cl, 14.94; N, 8.86; O, 10.12; S, 6.76
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CAS # |
113559-13-0
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Related CAS # |
113558-89-7;113559-13-0 (2HCl);
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Appearance |
Solid powder
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SMILES |
CS(=O)(NC1=CC=C(C(C2CCN(CCC3=NC(C)=CC=C3)CC2)=O)C=C1)=O.[H]Cl.[H]Cl
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InChi Key |
ZQBNWMFBOSOOLX-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C21H27N3O3S.2ClH/c1-16-4-3-5-19(22-16)12-15-24-13-10-18(11-14-24)21(25)17-6-8-20(9-7-17)23-28(2,26)27;;/h3-9,18,23H,10-15H2,1-2H3;2*1H
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Chemical Name |
N-[4-[1-[2-(6-methylpyridin-2-yl)ethyl]piperidine-4-carbonyl]phenyl]methanesulfonamide dihydrochloride
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Synonyms |
E-4031; E4031; E 4031; E4031 2HCl; E-4031 dihydrochloride
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
H2O : ≥ 50 mg/mL (~105.39 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (210.77 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
 (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.1077 mL | 10.5387 mL | 21.0775 mL | |
5 mM | 0.4215 mL | 2.1077 mL | 4.2155 mL | |
10 mM | 0.2108 mL | 1.0539 mL | 2.1077 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.