5.08317

A740003

• Sinónimos: A740003, N-(1-{[(cyanoimino)(5-quinolinylamino) methyl] amino}-2,2-dimethylpropyl)-2-(3,4-dimethoxyphenyl)acetamide, A 740003, P2X7 Purinegic Receptor, A740003, A740003
• Fórmula empírica (notación de Hill): C₂₆H₃₀N₆O₃
• Número de CAS: 861393-28-4
• Peso molecular: 474.55
• Número MDL: MFCD09970333
• Código UNSPSC: 12352200

Propiedades

• Ensayo: ≥98% (HPLC)
• Nivel de calidad: 100
• Formulario: powder
• potencia: 18 nM IC₅₀
• fabricante / nombre comercial: Calbiochem^®
• condiciones de almacenamiento: OK to freeze; protect from light
• color: off-white
• solubilidad: DMSO: 30 mg/mL
• temp. de almacenamiento: 2-8°C
• InChI: 1S/C26H30N6O3/c1-26(2,3)24(31-23(33)15-17-11-12-21(34-4)22(14-17)35-5)32-25(29-16-27)30-20-10-6-9-19-18(20)8-7-13-28-19/h6-14,24H,15H2,1-5H3,(H,31,33)(H2,29,30,32)
• Clave InChI: PUHSRMSFDASMAE-UHFFFAOYSA-N

Descripción

Descripción general

A highly potent, selective, competitive antagonist of P2X7 purinegic receptor (IC₅₀ = 18 nM and 40 nM, respectively as measured by Bz-ATP-stimulated Ca2+ flux). Does not affect other P2 receptors even at 10 µM concentrations. Blocks agonist-evoked IL-1b release (IC₅₀ = 156 nM) and pore formation (IC₅₀ = 92 nM) in differentiated human THP-1 cells. Also shown to reduce carrageenan and Freund′s adjuvant -induced thermal hyperalgesia (ED₅₀ = 38-54 mg/kg, i.p) and neuropathic pain induced by chronic constriction injury (CIC) of the sciatic nerve.

Acciones bioquímicas o fisiológicas

Primary Target
P2X7

Envase

Packaged under inert gas

Advertencia

Toxicity: Standard Handling (A)

Nota de preparación

Slight warming is required for complete solubilization.

Reconstitución

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

Otras notas

Honore, P., et al. 2006. J. Pharmacol. Exp. Ther.319, 1376.

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