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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-P2X Receptor-A-740003
A-740003

Chemical Structure : A-740003

CAS No.: 861393-28-4

A-740003 (A 740003, A740003)

货号: PC-45846Not For Human Use, Lab Use Only.

A-740003 (A740003) is a potent, selective, competitive P2X7 receptor antagonist with IC50 of 40 nM and 18 nM for hP2X7 and rP2X7, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

A-740003 (A740003) is a potent, selective, competitive P2X7 receptor antagonist with IC50 of 40 nM and 18 nM for hP2X7 and rP2X7, respectively.
A-740003 showed weak or no activity for other P2 receptors (IC50>10 uM); potently blocks agonist-evoked IL-1β release (IC50=156 nM) and pore formation (IC50=92 nM) in differentiated human THP-1 cells.
A-740003 produces dose-dependent antinociception in a spinal nerve ligation model (ED50=19 mg/kg i.p.) in the rat.

物理化学性质&存储条件

分子量 474.5548
分子式 C26H30N6O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Benzeneacetamide, N-[1-[[(cyanoamino)(5-quinolinylimino)methyl]amino]-2,2-dimethylpropyl]-3,4-dimethoxy-

参考文献

1. Honore P, et al. J Pharmacol Exp Ther. 2006 Dec;319(3):1376-85.

2. Morytko MJ, et al. Bioorg Med Chem Lett. 2008 Mar 15;18(6):2093-6.

3. King BF. Br J Pharmacol. 2007 Jul;151(5):565-7.

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