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Description

A xanthine derivative that serves as a fast acting, reversible, and selective activator of Kir6.2/SUR1 channels (EC50 = 7 µ,M). Directly occupies the binding site located within SUR1. Shown to be a more potent activator of Kir6.2/SUR1 than diazoxide (EC50 = 120 µ,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 µ,M) and exhibits very weak inhibitory activity against Kir3.1/3.2 (IC50 = 65 µ,M) and Kir2.3 (IC50 = 91 µ,M) channels. Inhibits glucose-stimulated Ca2+ influx into mouse pancreatic beta-cells., A xanthine derivative that serves as a fast acting, reversible, and selective activator of Kir6.2/SUR1 channels (EC50 = 7 µ,M). Directly occupies the binding site located within SUR1. Shown to be a more potent activator of Kir6.2/SUR1 than diazoxide (EC50 = 120 µ,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 µ,M) and exhibits very weak inhibitory activity against Kir3.1/3.2 (IC50 = 65 µ,M) and Kir2.3 (IC50 = 91 µ,M) channels. Inhibits glucose-stimulated Ca2+ influx into mouse pancreatic beta-cells.Please note that the molecular weight for this compound is batch-specific due to variable water content.