5.08317

A740003

• Synonym(e): A740003, N-(1-{[(cyanoimino)(5-quinolinylamino) methyl] amino}-2,2-dimethylpropyl)-2-(3,4-dimethoxyphenyl)acetamide, A 740003, P2X7 Purinegic Receptor, A740003, A740003
• Empirische Formel (Hill-System): C₂₆H₃₀N₆O₃
• CAS-Nummer: 861393-28-4
• Molekulargewicht: 474.55
• MDL-Nummer: MFCD09970333
• UNSPSC-Code: 12352200

Eigenschaften

• Assay: ≥98% (HPLC)
• Qualitätsniveau: 100
• Form: powder
• Wirksamkeit: 18 nM IC₅₀
• Hersteller/Markenname: Calbiochem^®
• Lagerbedingungen: OK to freeze; protect from light
• Farbe: off-white
• Löslichkeit: DMSO: 30 mg/mL
• Lagertemp.: 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)
• InChIKey: PUHSRMSFDASMAE-UHFFFAOYSA-N

Beschreibung

Allgemeine Beschreibung

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.

Biochem./physiol. Wirkung

Primary Target
P2X7

Verpackung

Packaged under inert gas

Warnhinweis

Toxicity: Standard Handling (A)

Angaben zur Herstellung

Slight warming is required for complete solubilization.

Rekonstituierung

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

Sonstige Hinweise

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

Rechtliche Hinweise

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

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable