Biochem/physiol Actions

Reversible: yes

EC₅₀ = 7 µM for Kir6.2/SUR1 channel activation

Primary TargetSUR1-containing channels

General description

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.

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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Raphemot, R., et al. 2014. Mol. Pharmacol.85, 858.

Packaging

Packaged under inert gas

10 mg in Glass bottle

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Warning

Toxicity: Standard Handling (A)