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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-Calcium Channel -VK-II-86
VK-II-86

Chemical Structure : VK-II-86

CAS No.: 955371-84-3

VK-II-86 (RyR2 inhibitor)

货号: PC-38485Not For Human Use, Lab Use Only.

VK-II-86 is a carvedilol analogue lacking antagonist activity at β-adrenoceptors, effectively suppresses SOICR by directly reducing the open duration of the cardiac ryanodine receptor (RyR2).

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

VK-II-86 is a carvedilol analogue lacking antagonist activity at β-adrenoceptors, effectively suppresses SOICR by directly reducing the open duration of the cardiac ryanodine receptor (RyR2).
VK-II-86 exhibited >2,000-fold lower beta-AR binding affinity than carvedilol.
VK-II-86 prevented stress-induced ventricular tachyarrhythmias in RyR2-mutant mice and did so more effectively when combined with either of the selective beta blockers metoprolol or bisoprolol.
VK-II-86 prevented hypokalaemia-induced AP prolongation and depolarization but did not alter AP parameters in normokalaemia.

物理化学性质&存储条件

分子量 420.5
分子式 C25H28N2O4
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-(9H-Carbazol-4-yloxy)-1-[[2-(2-methoxyphenoxy)ethyl]amino]-2-butanol

参考文献

1. Zhou Q, et al. Nat Med. 2011 Jul 10;17(8):1003-9.

2. Gonano LA, et al. Circ J. 2018 Dec 25;83(1):41-51.

3. Robinson VM, et al. Br J Pharmacol. 2021 Dec 7. doi: 10.1111/bph.15775.

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