KIR6.2/SUR1 CHANNEL ACTIVATOR VU0071063 (C15-1305-034)

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 activation

Primary Target
SUR1-containing channels

Reversible: 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.

Legal Information

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

Molecular Weight: 326.39. Empirical Formula: C₁₈H₂₂N₄O₂. 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. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.