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VK-II-86

目录号 : GC90516

SOICR的抑制剂。

VK-II-86 Chemical Structure

Cas No.:955371-84-3

规格 价格 库存 购买数量
1 mg
¥505.00
现货
5 mg
¥2,278.00
现货
10 mg
¥4,038.00
现货
25 mg
¥8,205.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

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产品描述

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

Chemical Properties

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
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溶解性数据

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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
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