492031

NS8593

An aminobenzimidazole derivative that selectively and reversibly blocks small conductance Ca2+-activated K+ channels in a Ca2+-dependent manner.

• 同義詞: NS8593, (R)-N-(Benzimidazol-2-yl)-1,2,3,4-tetrahydro-1-naphthylamine
• 經驗公式（希爾表示法）: C₁₇H₁₇N₃
• CAS號碼: 875755-39-8
• 分子量：: 263.34
• MDL號碼: MFCD32671885
• 分類程式碼代碼: 12352200
• NACRES: NA.77

屬性

• 品質等級: 100
• 化驗: ≥98% (HPLC)
• 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
• 運輸包裝: wet ice
• 儲存溫度: 2-8°C
• SMILES 字串: C1(NC(N[C@@H]2CCCC3=C2C=CC=C3)=N4)=C4C=CC=C1

描述

一般說明

An aminobenzimidazole derivative that selectively and reversibly blocks small conductance Ca2+-activated K+ channels (SK1-3; K_d = 420 nM, 600 nM, and 730 nM for SK1, SK2, SK3, respectively) in a Ca2+-dependent manner. It mediates channel gating by interacting with gating structures deep within the inner pore vestibule where Ser507 and Ala532 are deemed to be important for inhibition. Interacts at a site that is distinct from the apamin binding site in SK channels. Can access high-affinity binding sites from both the inside and outside of the cell membrane. Does not affect QT intervals, but prolongs the atrial effective refractive period and prevents acetylcholine-induced atrial fibrillations in ex vivo and in vivo models. Also shown to reversibly block TRPM7 channel (IC₅₀ = 1.6 mM) in smooth muscle cells, primary podocytes, HEK293 cells expressing TRPM7, and ventricular myocytes in a Mg2+-dependent manner and blocks the motility of cells in culture.

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 3 months at -20°C.

其他說明

Chubanov, V., et al. 2012. Brit. Journ. Pharm.166, 1357.
Jenkins, D., et al. 2011. Hypertension.57, 1129.
Jenkins, D., et al. 2011. Mol. Pharm.79, 899.
Jenkins, D., et al. 2011. Mol. Pharm.79, 899.
Lasse, S., et al. 2011. J. Cardiov. Pharm.57, 672.
Diness, J., et al. 2010. Circ Arrhythm Electrophusiol.3, 380.
Ji, H., et al. 2009. Eur. J. Neurosci.9, 1883.
Strobaek, D., et al. 2006. Mol. Pharm.70, 1771.

法律資訊

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

安全資訊

• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 2