Sigma-Aldrich Kir6.2/Sur1 Channel Activa

Assay

≥97% (HPLC)

Quality Level

100

Form

powder

Manufacturer/Tradename

Calbiochem^®

Storage Condition

OK to freeze
protect from light

Color

white

Solubility

DMSO: 100 mg/mL

Storage Temp.

2-8°C

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.

Biochem/Physiol Actions

EC₅₀= 7 µM for Kir6.2/SUR1 channel activationPrimary Target
SUR1-containing channelsReversible: yes

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Other Notes

Raphemot, R., et Al. 2014.Mol. Pharmacol. 85,858.CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany