5.30923

Kir6.2/SUR1 Channel Activator, VU0071063

• Synonym(e): Kir6.2/SUR1 Channel Activator, VU0071063, 1,3-Dimethyl-7-(4-(2-methyl-2-propanyl)benzyl)-3,7-dihydro-1H-purine-2,6-dione, 7-(4-( tert-Butyl)benzyl)-1,3-dimethyl-1H-purine-2,6(3H,7H)-dione, Kir6.2/SUR1 Channel Opener, SUR1/Kir6.2 selective K-ATP Channel Opener, 1,3-Dimethyl-7-(4-(2-methyl-2-propanyl)benzyl)-3,7-dihydro-1H-purine-2,6-dione, 7-(4-(tert-Butyl)benzyl)-1,3-dimethyl-1H-purine-2,6(3H,7H)-dione, Kir6.2/SUR1 Channel Opener, SUR1/Kir6.2 selective K-ATP Channel Opener
• Empirische Formel (Hill-System): C₁₈H₂₂N₄O₂
• CAS-Nummer: 333415-38-6
• Molekulargewicht: 326.39
• MDL number: MFCD02648040
• UNSPSC Code: 12352200
• NACRES: NA.77
• Assay: ≥97% (HPLC)
• Form: powder
• Storage condition: OK to freeze, protect from light

Eigenschaften

• 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

Beschreibung

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)

Sicherheitshinweise

• Lagerklasse: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable