5.08317

A740003

• 別名: A740003, N-(1-{[(cyanoimino)(5-quinolinylamino) methyl] amino}-2,2-dimethylpropyl)-2-(3,4-dimethoxyphenyl)acetamide, A 740003, P2X7 Purinegic Receptor, A740003, A740003
• 実験式（ヒル表記法）: C₂₆H₃₀N₆O₃
• CAS番号: 861393-28-4
• 分子量: 474.55
• MDL番号: MFCD09970333
• UNSPSCコード: 12352200

特性

• アッセイ: ≥98% (HPLC)
• 品質水準: 100
• 形状: powder
• 有効性: 18 nM IC₅₀
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: off-white
• 溶解性: DMSO: 30 mg/mL
• 保管温度: 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)
• InChI Key: PUHSRMSFDASMAE-UHFFFAOYSA-N

詳細

詳細

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.

生物化学的／生理学的作用

Primary Target
P2X7

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

調製ノート

Slight warming is required for complete solubilization.

再構成

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

その他情報

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

法的情報

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

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable