492031

NS8593

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

• Sinónimos: NS8593, (R)-N-(Benzimidazol-2-yl)-1,2,3,4-tetrahydro-1-naphthylamine
• Fórmula empírica (notación de Hill): C₁₇H₁₇N₃
• Número de CAS: 875755-39-8
• Peso molecular: 263.34
• Número MDL: MFCD32671885
• Código UNSPSC: 12352200
• NACRES: NA.77

Propiedades

• Nivel de calidad: 100
• Análisis: ≥98% (HPLC)
• formulario: powder
• fabricante / nombre comercial: Calbiochem^®
• condiciones de almacenamiento: OK to freeze; protect from light
• color: white
• solubilidad: DMSO: 100 mg/mL
• Condiciones de envío: wet ice
• temp. de almacenamiento: 2-8°C
• cadena SMILES: C1(NC(N[C@@H]2CCCC3=C2C=CC=C3)=N4)=C4C=CC=C1

Descripción

Descripción general

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.

Envase

Packaged under inert gas

Advertencia

Toxicity: Standard Handling (A)

Reconstitución

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Otras notas

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.

Información legal

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

Información de seguridad

• Código de clase de almacenamiento: 11 - Combustible Solids
• Clase de riesgo para el agua (WGK): WGK 2