产品说明
一般描述
A xanthine derivative that serves as a fast acting, reversible, and selective activator of Kir6.2/SUR1 channels (EC50 = 7 µM). Directly occupies the binding site located within SUR1. Shown to be a more potent activator of Kir6.2/SUR1 than diazoxide (EC50 = 120 µM). However, it does not affect Kir6.1/SURA2A or Kir6.2/SURA2A channels and is inactive against Kir2.1 and Kir2.2 (IC50 >100 µM) and exhibits very weak inhibitory activity against Kir3.1/3.2 (IC50 = 65 µM) and Kir2.3 (IC50 = 91 µM) channels. Inhibits glucose-stimulated Ca2+ influx into mouse pancreatic β-cells.
Please note that the molecular weight for this compound is batch-specific due to variable water content.
A xanthine derivative that serves as a fast acting, reversible, and selective activator of Kir6.2/SUR1 channels (EC50 = 7 µM). Directly occupies the binding site located within SUR1. Shown to be a more potent activator of Kir6.2/SUR1 than diazoxide (EC50 = 120 µM). However, it does not affect Kir6.1/SURA2A or Kir6.2/SURA2A channels and is inactive against Kir2.1 and Kir2.2 (IC50 >100 µM) and exhibits very weak inhibitory activity against Kir3.1/3.2 (IC50 = 65 µM) and Kir2.3 (IC50 = 91 µM) channels. Inhibits glucose-stimulated Ca2+ influx into mouse pancreatic β-cells.
生化/生理作用
Primary Target
SUR1-containing channels
EC50 = 7 µM for Kir6.2/SUR1 channel activation
Reversible: yes
包装
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
其他说明
Raphemot, R., et al. 2014. Mol. Pharmacol.85, 858.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
基本信息
经验(实验)分子式 | C18H22N4O2 |
分子量 | 326.39 |
产品性质
质量水平 | 100 |
测定 | ≥97% (HPLC) |
形式 | powder |
manufacturer/tradename | Calbiochem® |
储存条件 | OK to freeze protect from light |
颜色 | white |
溶解性 | DMSO: 100 mg/mL |
储存温度 | 2-8℃ |
安全信息
储存分类代码 | 11 - Combustible Solids |
WGK | WGK 3 |
闪点(F) | Not applicable |
闪点(C) | Not applicable |
Sigma-Aldrich