GS967|cas:1262618-39-2|西域试剂

GS967,99.95%

产品编号：Bellancom-12593| CAS NO：1262618-39-2| 分子式：C₁₄H₇F₆N₃O| 分子量：347.22

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-12593	￥550.00	杭州北京（现货）
Bellancom-12593	￥850.00	杭州北京（现货）
Bellancom-12593	￥3650.00	杭州北京（现货）
Bellancom-12593	￥6400.00	杭州北京（现货）
Bellancom-12593	￥11000.00	杭州北京（现货）

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GS967

产品介绍

GS967 (GS-458967)是有效地选择性的心脏晚期钠电流抑制剂（late I_Na），在心室肌细胞和心脏中的IC₅₀值分别为0.13和0.21 μM。

生物活性

GS967 (GS-458967) is a potent, and selective inhibitor of cardiac late sodium current (late I_Na ) with IC₅₀ values of 0.13 and 0.21 μM for ventricular myocytes and isolated hearts, respectively.

体外研究

GS967 (10, 100, 300 nM) completely attenuates the effect of ATX-II (10 nM) to increase action potential duration (APD) and APD variability in ventricular myocytes, with an apparent IC₅₀ value of ∼10 nM and decreased the beat-to-beat variability of APD.

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

体内研究

GS967 prevents and reverses proarrhythmic effects of the late I_Na enhancer ATX-II and the I_Kr inhibitor E-4031. GS967 significantly attenuates the proarrhythmic effects of methoxamine 1 clofilium and suppressed ischemia-induced arrhythmias. GS967 causes a reduction of I_NaP in a frequency-dependent manner, consistent with use-dependent block (UDB). GS967 evokes more potent UDB of I_NaP (IC₅₀=0.07 μM) than ranolazine (16 μM) and lidocaine (17 μM). GS967 is found to exert these same effects on a prototypical long QT syndromemutation (delKPQ). GS967 prevents ischemia-induced increases in alternans in the left atrium and left ventricle. GS967 reduces ischemia-induced increases in depolarization heterogeneity and repolarizationheterogeneity. GS967 does not alter heart rate, arterial blood pressure, PR and QT intervals, or QRS duration, but it mildly decreased contractility during ischemia, which was consistent with late INa inhibition.

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

体内研究

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

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (144.00 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.8800 mL	14.4001 mL	28.8002 mL
5 mM	0.5760 mL	2.8800 mL	5.7600 mL
10 mM	0.2880 mL	1.4400 mL	2.8800 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。-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 (7.20 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (7.20 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
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% corn oil
Solubility: ≥ 2.5 mg/mL (7.20 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.20 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。