Kir6.2/SUR1 Channel Activator, VU0071063-Calbiochem

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一般描述

A xanthine derivative that serves as a fast acting, reversible, and selective activator of Kir6.2/SUR1 channels (EC₅₀= 7 ?M). Directly occupies the binding site located within SUR1. Shown to be a more potent activator of Kir6.2/SUR1 than diazoxide (EC₅₀= 120 ?M). However, it does not affect Kir6.1/SURA2A or Kir6.2/SURA2A channels and is inactive against Kir2.1 and Kir2.2 (IC₅₀>100 ?M) and exhibits very weak inhibitory activity against Kir3.1/3.2 (IC₅₀= 65 ?M) and Kir2.3 (IC₅₀= 91 ?M) 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 ?M). Directly occupies the binding site located within SUR1. Shown to be a more potent activator of Kir6.2/SUR1 than diazoxide (EC₅₀= 120 ?M). However, it does not affect Kir6.1/SURA2A or Kir6.2/SURA2A channels and is inactive against Kir2.1 and Kir2.2 (IC₅₀>100 ?M) and exhibits very weak inhibitory activity against Kir3.1/3.2 (IC₅₀= 65 ?M) and Kir2.3 (IC₅₀= 91 ?M) channels. Inhibits glucose-stimulated Ca²⁺influx into mouse pancreatic β-cells.

生化/生理作用

Primary Target
SUR1-containing channels
EC₅₀= 7 ?M 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

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