VK-II-86
目录号 : GC90516SOICR的抑制剂。
Cas No.:955371-84-3
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >90.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
VK-II-86 is an inhibitor of store-overload-induced calcium release (SOICR) and a derivative of carvedilol .1 It inhibits SOICR in HEK293 cells expressing the ryanodine receptor 2 (RyR2) R4496C (RyR2R4496C) mutation (IC50 = 16.8 µM), a mutation that results in spontaneous calcium release from the endoplasmic reticulum. VK-II-86 (1 µM) inhibits the inward-rectifier potassium channel 2.1 (Kir2.1), cardiac late sodium current (late INa), and L-type calcium current (ICa) in isolated canine cardiomyocytes and delayed-rectifier potassium current (IKr) in HEK293 cells expressing human-ether-a-go-go (hERG), also known as Kv11.1, in pokalaemic, but not normokalaemic, conditions.2 It is also an antagonist of toll-like receptor 4 (TLR4; IC50 = 32.55 µM in HEK293 cells expressing the human receptor) and inhibits perpolarization-activated cyclic nucleotide gated potassium channel 4 (HCN4) in COS-7 cells expressing HCN4 when used at a concentration of 10 µM.3 VK-II-86 prevents pokalaemia-induced ventricular arrthmia in isolated Langendorff-perfused mouse hearts.2 Unlike the β-adrenergic receptor antagonist carvedilol, it does not reverse isoproterenol-induced increases in heart rate or decrease resting heart rate in RyR2R4496C-expressing mice.4
Cas No. | 955371-84-3 | SDF | |
分子式 | C25H28N2O4 | 分子量 | 420.5 |
溶解度 | DMSO : 100 mg/mL (237.81 mM; Need ultrasonic) | 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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.3781 mL | 11.8906 mL | 23.7812 mL |
5 mM | 0.4756 mL | 2.3781 mL | 4.7562 mL |
10 mM | 0.2378 mL | 1.1891 mL | 2.3781 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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。