Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GS967 是一种有效的、选择性的心脏晚期钠电流(late I Na)抑制剂,心室肌细胞和心脏中的IC50分别为0.13和0.21 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 283 | 现货 | ||
5 mg | ¥ 455 | 现货 | ||
10 mg | ¥ 690 | 现货 | ||
25 mg | ¥ 1,470 | 现货 | ||
50 mg | ¥ 2,780 | 现货 | ||
100 mg | ¥ 4,250 | 现货 | ||
200 mg | ¥ 6,290 | 现货 | ||
500 mg | ¥ 9,480 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 493 | 现货 |
产品描述 | GS967 is a potent, and selective inhibitor of cardiac late sodium current (late INa ). |
靶点活性 | Late INa:0.13 μM |
体外活性 | 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[1]. |
体内活性 | GS967 prevents and reverses proarrhythmic effects of the late INa enhancer ATX-II and the IKr inhibitor E-4031. GS967 significantly attenuates the proarrhythmic effects of methoxamine 1 clofilium and suppressed ischemia-induced arrhythmias[1]. GS967 causes a reduction of INaP in a frequency-dependent manner, consistent with use-dependent block (UDB). GS967 evokes more potent UDB of INaP (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)[2]. 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[3]. |
激酶实验 | The IC50 of LY-364947 at different enzyme concentrations are determined by the filter-binding assay. Typically, 40 μL reactions in 50 mM HEPES at pH 7.5, 1 mM NaF, 200 μM pKSmad3(-3), and 50 mM ATP containing a titration of each inhibitor with concentrations of 1600, 800, 400, 200, 100, 50, 25, and 0 nM are incubated at 30°C for 30 min. The IC50 is calculated using a nonlinear regression method with GraphPad Prism software. The binding type is determined by plotting the correlation between enzyme concentrations and IC50 values. |
别名 | GS458967 |
分子量 | 347.22 |
分子式 | C14H7F6N3O |
CAS No. | 1262618-39-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (144 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.88 mL | 14.4001 mL | 28.8002 mL | 72.0005 mL |
5 mM | 0.576 mL | 2.88 mL | 5.76 mL | 14.4001 mL | |
10 mM | 0.288 mL | 1.44 mL | 2.88 mL | 7.2 mL | |
20 mM | 0.144 mL | 0.72 mL | 1.44 mL | 3.6 mL | |
50 mM | 0.0576 mL | 0.288 mL | 0.576 mL | 1.44 mL | |
100 mM | 0.0288 mL | 0.144 mL | 0.288 mL | 0.72 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
GS967 1262618-39-2 Membrane transporter/Ion channel Sodium Channel GS 967 inhibit GS 458967 GS458967 Na+ channels GS-967 Na channels GS-458967 Inhibitor inhibitor