GS967
目录号 : GC10830
A selective inhibitor of cardiac late sodium current
Cas No.:1262618-39-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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Animal experiment: |
Rats: Ventricular tachycardia or fibrillation are induced either by local aconitine injection (50 μg) in the left ventricular muscle of adult male rats or by arterial perfusion of 0.1 mM hydrogen peroxide in aged male rats. The left ventricular epicardial surface of the isolated-perfused hearts is optically mapped using fluorescent voltage-sensitive dye, and microelectrode recordings of action potentials are made adjacent to the aconitine injection site. The suppressive and preventive effects of GS967 (1 μM) against EAD/DAD-mediated ventricular tachycardia or fibrillation are then determined[2]. Rabbits: To determine the effect of GS967 on the inducibility of TdP by clofilium in the presence of methoxamine, rabbits are first treated with either vehicle or GS967 (in randomized manner) given as a 60 μg/kg bolus, followed by a 16 μg/kg/min infusion that is maintained for the duration of an experiment. After 10 minutes, methoxamine is infused intravenously at 15 μg/kg/min, followed 10 minutes later by clofilium at 100 nmol/kg/min. The incidences of premature ventricular contractions (PVCs), ventricular tachycardia (VT; defined as three or more consecutive abnormal beats), and TdP are determined from the ECG recordings[1]. |
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References: [1]. Belardinelli L, et al. A novel, potent, and selective inhibitor of cardiac late sodium current suppresses experimental arrhythmias. J Pharmacol Exp Ther. 2013 Jan;344(1):23-32. |
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GS967 is a potent, selective and novel inhibitor of cardiac late sodium current (late INa) with IC50=0.13 μM in ventricular myocytes and IC50=0.21μM in isolated hearts. [1]
When Na+ channels in myocytes fail to inactivate after opening, Na+ influx continues throughout the AP plateau. The resulting Na+ current (INa) is referred to as late INa. Its magnitude is increased in many pathologic conditions, such as in the failing and/or ischemic heart, in the heart exposed to oxidative stress, and in hearts of patients with congenital long QT3 syndromes. [1]
In rabbit isolated ventricular myocytes, inhibition of peak INa by GS967 is in a concentration- and voltage-dependent manner with minimal use-dependent, it also decreases the Na+ and Ca2+ overload. In rabbit-isolated heart, GS967 abolishes TdP Induced by ATX-II or E-4031. [1]
In anesthetized rabbit, GS967 reduces MAPD90 but did not alter cardiac conduction time; it also prevents the Induction of arrhythmic activity and TdP by clofilium and decreases the Incidence of ischemia-Induced arrhythmias. [1]
Reference:
1. Belardinelli L, Liu G, Smith-Maxwell C et al. A novel, potent, and selective inhibitor of
cardiac late sodium current suppresses experimental arrhythmias. J Pharmacol Exp
Ther. 2013 Jan;344(1):23-32.
| Cas No. | 1262618-39-2 | SDF | |
| 化学名 | 6-(4-(trifluoromethoxy)phenyl)-3-(trifluoromethyl)-[1,2,4]triazolo[4,3-a]pyridine | ||
| Canonical SMILES | FC(F)(F)C1=NN=C2C=CC(C3=CC=C(OC(F)(F)F)C=C3)=CN21 | ||
| 分子式 | C14H7F6N3O | 分子量 | 347.22 |
| 溶解度 | ≥ 13.35mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.88 mL | 14.4001 mL | 28.8002 mL |
| 5 mM | 0.576 mL | 2.88 mL | 5.76 mL |
| 10 mM | 0.288 mL | 1.44 mL | 2.88 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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