5.30923

Kir6.2/SUR1 Channel Activator, VU0071063

• 別名: 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
• 実験式（ヒル表記法）: C₁₈H₂₂N₄O₂
• CAS番号: 333415-38-6
• 分子量: 326.39
• MDL番号: MFCD02648040
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• アッセイ: ≥97% (HPLC)
• 品質水準: 100
• フォーム: powder
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: white
• 溶解性: DMSO: 100 mg/mL
• 保管温度: 2-8°C
• SMILES記法: [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

詳細

詳細

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.

生物化学的／生理学的作用

EC₅₀ = 7 µM for Kir6.2/SUR1 channel activation

Primary Target
SUR1-containing channels

Reversible: yes

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

再構成

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

その他情報

Raphemot, R., et al. 2014. Mol. Pharmacol.85, 858.

法的情報

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

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable