Eleclazine hydrochloride GS 6615 hydrochloride|cas:1448754-43-5|西域试剂

Eleclazine hydrochloride GS 6615 hydrochloride,99.62%

产品编号：Bellancom-16738A| CAS NO：1448754-43-5| 分子式：C₂₁H₁₇ClF₃N₃O₃| 分子量：451.83

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货号	价格	库存与货期
Bellancom-16738A	￥3000.00	杭州北京（现货）
Bellancom-16738A	￥4500.00	杭州北京（现货）
Bellancom-16738A	￥13500.00	杭州北京（现货）

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Eleclazine hydrochloride GS 6615 hydrochloride

产品介绍

Eleclazine (GS 6615) hydrochloride 是一种具有选择性的心脏晚期钠电流 (sodium current) 抑制剂和钾电流 (potassium current) 的弱抑制剂，IC₅₀ 值分别为 <1 μM 和约 14.2 μM。在猪模型中，Eleclazine hydrochloride 对自发性心房早搏、复极交替和异质性以及心房纤颤同时具有保护作用。Eleclazine hydrochloride 可用于心律失常的研究。

生物活性

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.

体外研究

Eleclazine inhibits sodium current in hiPSC-derived cardiomyocytes with an IC₅₀ of 2.5 μM.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (110.66 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2132 mL	11.0661 mL	22.1322 mL
5 mM	0.4426 mL	2.2132 mL	4.4264 mL
10 mM	0.2213 mL	1.1066 mL	2.2132 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (5.53 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.53 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (5.53 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.53 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.53 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.53 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。