5.08317

A740003

• 同義詞: A740003, N-(1-{[(cyanoimino)(5-quinolinylamino) methyl] amino}-2,2-dimethylpropyl)-2-(3,4-dimethoxyphenyl)acetamide, A 740003, P2X7 Purinegic Receptor, A740003, A740003
• 經驗公式（希爾表示法）: C₂₆H₃₀N₆O₃
• CAS號碼: 861393-28-4
• 分子量：: 474.55
• MDL號碼: MFCD09970333
• 分類程式碼代碼: 12352200

屬性

• 化驗: ≥98% (HPLC)
• 品質等級: 100
• 形狀: powder
• 效力: 18 nM IC₅₀
• 製造商／商標名: Calbiochem^®
• 儲存條件: OK to freeze; protect from light
• 顏色: off-white
• 溶解度: DMSO: 30 mg/mL
• 儲存溫度: 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 密鑰: PUHSRMSFDASMAE-UHFFFAOYSA-N

描述

一般說明

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.

生化／生理作用

Primary Target
P2X7

包裝

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

準備報告

Slight warming is required for complete solubilization.

重構

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

其他說明

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

法律資訊

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

安全資訊

• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 3
• 閃點（°F）: Not applicable
• 閃點（°C）: Not applicable