5.08317

A740003

• Synonyme(s) : A740003, N-(1-{[(cyanoimino)(5-quinolinylamino) methyl] amino}-2,2-dimethylpropyl)-2-(3,4-dimethoxyphenyl)acetamide, A 740003, P2X7 Purinegic Receptor, A740003, A740003
• Formule empirique (notation de Hill): C₂₆H₃₀N₆O₃
• Numéro CAS: 861393-28-4
• Poids moléculaire : 474.55
• Numéro MDL: MFCD09970333
• Code UNSPSC : 12352200

Propriétés

• Pureté: ≥98% (HPLC)
• Niveau de qualité: 100
• Forme: powder
• Puissance: 18 nM IC₅₀
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: off-white
• Solubilité: DMSO: 30 mg/mL
• Température de stockage: 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)
• Clé InChI: PUHSRMSFDASMAE-UHFFFAOYSA-N

Description

Description générale

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.

Actions biochimiques/physiologiques

Primary Target
P2X7

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Notes préparatoires

Slight warming is required for complete solubilization.

Reconstitution

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

Autres remarques

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

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable