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)
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