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.
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
Preparation Note
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
Disclaimer
Toxicity: Standard Handling (A)
| assay | ≥97% (HPLC) |
| Quality Segment | 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 |
| SMILES string | [n]1(c2nc[n](c2[c]([n]([c]1=O)C)=O)Cc3ccc(cc3)C(C)(C)C)C |
| InChI | 1S/C18H22N4O2/c1-18(2,3)13-8-6-12(7-9-13)10-22-11-19-15-14(22)16(23)21(5)17(24)20(15)4/h6-9,11H,10H2,1-5H3 |
| InChI key | ZFZAIHKQJBMYLO-UHFFFAOYSA-N |
