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• 產(chǎn)品描述： Eleclazine (GS 6615) hydrochloride is a selective cardiac late sodium current inhibitor and a weak inhibitor of potassium current with IC50 value of <1 μM and approximately 14.2 μM, respectively. Eleclazine hydrochloride shows concurrent protection against autonomically induced atrial premature beats, repolarization alternans and heterogeneity, and atrial fibrillation in porcine model. Eleclazine hydrochloride can be used to research cardiac arrhythmias

• 靶點(diǎn)： Sodium current, Potassium current;SodiumChannel

• 體外研究：
  Eleclazine inhibits sodium current in hiPSC-derived cardiomyocytes with an IC50 of 2.5 μM

• 體內(nèi)研究：
  Eleclazine (0.3 and 0.9 mg/kg; IV; infused over 15 minutes) reduces the incidence of epinephrine-induced ventricular premature beats and couplets, and shortens ventricular QT and atrial PTa intervals. Animal Model: Male Yorkshire pigs (35.20 ± 0.46 kg; injected with epinephrine via a jugular vein) Dosage: 0.3 and 0.9 mg/kg Administration: IV; infused over 15 minutes Result: Reduced the incidence of epinephrine-induced ventricular premature beats and couplets by 51% (from 31.3 ± 1.91 to 15.2 ± 5.08 episodes; P = 0.038) and the incidence of 3- to 7-beat ventricular tachycardia (VT) by 56% (from 10.8 ± 3.45 to 4.7 ± 3.12 episodes; P = 0.004).Shortened ventricular QT and atrial PTa intervals by 7%, and reduced atrial repolarization alternans and heterogeneity without attenuation of the inotropic response to catecholamine.

• 參考文獻(xiàn)：
  1. Bacic D, et al. Eleclazine, an inhibitor of the cardiac late sodium current, is superior to flecainide in suppressing catecholamine-induced ventricular tachycardia and T-wave alternans in an intact porcine model. Heart Rhythm. 2017 Mar;14(3):448-454. 2. Rajamani S et al. The novel late Na+ current inhibitor, GS-6615 (eleclazine) and its anti-arrhythmic effects in rabbit isolated heart preparations. Br J Pharmacol. 2016 Jul 23. 3. Potet F, Egecioglu DE, Burridge PW, George AL Jr. GS-967 and Eleclazine Block Sodium Channels in Human Induced Pluripotent Stem Cell-Derived Cardiomyocytes. Mol Pharmacol. 2020 Nov;98(5):540-547.

• 溶解性： soluble  in  DMSO

• 保存條件： -20℃

• 配置溶液濃度參考：
  

  	1mg	5mg	10mg
  1 mM	2.213 ml	11.066 ml	22.132 ml
  5 mM	0.443 ml	2.213 ml	4.426 ml
  10 mM	0.221 ml	1.107 ml	2.213 ml
  50 mM	0.044 ml	0.221 ml	0.443 ml

• 注意：部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

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本計(jì)算器可幫助您計(jì)算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系，公式為：

質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *