5.30923

Kir6.2/SUR1 Channel Activator, VU0071063

• 别名: 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
• 经验公式（希尔记法）: C₁₈H₂₂N₄O₂
• CAS号: 333415-38-6
• 分子量: 326.39
• 分類程式碼代碼: 12352200
• NACRES: NA.77

属性

• 化驗: ≥97% (HPLC)
• 品質等級: 100
• 形狀: powder
• 製造商／商標名: Calbiochem^®
• 儲存條件: OK to freeze; protect from light
• 顏色: white
• 溶解度: DMSO: 100 mg/mL
• 儲存溫度: 2-8°C

说明

一般說明

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.

生化／生理作用

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

Primary Target
SUR1-containing channels

Reversible: yes

包裝

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重構

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

其他說明

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

法律資訊

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

安全信息

• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 3
• 閃點（°F）: Not applicable
• 閃點（°C）: Not applicable