420336-M

KB-R7943

• Sinónimos: KB-R7943, 2-(2-(4-(4-Nitrobenzyloxy)phenyl)ethyl)isothiourea, methane sulfonate, NMDA Antagonist III
• Fórmula empírica (notación de Hill): C₁₆H₁₇N₃O₃S · xCH₄O₃S
• Número de CAS: 182004-65-5
• Peso molecular: 331.39 (free base basis)
• Código UNSPSC: 12352200

Propiedades

• Análisis: ≥98% (HPLC)
• Nivel de calidad: 100
• formulario: crystalline solid
• fabricante / nombre comercial: Calbiochem^®
• condiciones de almacenamiento: OK to freeze; desiccated (hygroscopic); protect from light
• color: white
• solubilidad: water: 4 mg/mL; DMSO: 40 mg/mL
• temp. de almacenamiento: 2-8°C
• InChI: 1S/C16H17N3O3S.CH4O3S/c17-16(18)23-10-9-12-3-7-15(8-4-12)22-11-13-1-5-14(6-2-13)19(20)21;1-5(2,3)4/h1-8H,9-11H2,(H3,17,18);1H3,(H,2,3,4)
• Clave InChI: WGIKEBHIKKWJLG-UHFFFAOYSA-N

Descripción

Descripción general

A cell-permeable inhibitor of the influx/reverse mode of the Na⁺/Ca²⁺ exchanger (NCX) (IC₅₀ = 4.3 µM for NCX1, 4.7 µM for NCX2, and 1.4 µM for NCX3). Directly modulates Na⁺/Mg²⁺ exchange in a Ca²⁺-dependent manner. Reported ot offer neuronal and cardio-protection against ischemic injury. Also inhibits nicotinic acetylcholine receptors and NMDA receptor channels (IC₅₀<10 µM).

A cell-permeable isothiourea derivative that inhibits the influx/reverse mode of Na⁺/Ca²⁺ exchangers (NCX; IC₅₀ = 4.3 µM, 4.7 µM, and 1.4 µM for NCX1,NCX2, and NCX3, respectively) and directly modulates Na⁺/Mg²⁺ exchange in a Ca²⁺-dependent manner. Reported to offer neuronal and cardioprotection. Also inhibits nicotinic acetylcholine receptors and NMDA receptor channels (IC₅₀<10 µM).

Acciones bioquímicas o fisiológicas

Primary Target
Na+/Ca2+ exchangers

Target IC₅₀: 4.3 µM, 4.7 µM, and 1.4 µM for NCX1,NCX2, and NCX3, respectively

Advertencia

Toxicity: Irritant (B)

Reconstitución

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

Otras notas

Hobai, I.A., and O′Rourke, B. 2004. Expert Opin. Investig. Drugs13, 653.
Uetani, T., et al. 2003. J. Biol. Chem.278, 47491.
Iwamoto, T., et al. 2001. Mol. Pharmacol.59, 524.
Pintado, A.J., et al. 2000. Br. J. Pharmacol.130, 1893.
Sobolevsky, A.I., and Khodorov, B.I. 1999. Neuropharmacology38, 1235.
Iwamoto, T., et al. 1996. J. Biol. Chem.271, 22391.
Watano, T., et al. 1996. Br. J. Pharmacol.119, 555.

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 3
• Punto de inflamabilidad (°F): Not applicable
• Punto de inflamabilidad (°C): Not applicable