货号 | 3323/50 |
别名 | N-[2-[[2-[(2-Hydroxyethyl)amino]eth |
供应商 | Tocris |
生物活性 | Potent P2X7 receptor antagonist (KD values are 1.4 and 19 nM at human and rat P2X7 receptors respectively). Binds in a positive cooperative manner to sites distinct from, but coupled to, the ATP binding site and acts as a negative allosteric modulator. Inhibits tumor growth and displays antiangiogenic effects in mice. |
运输条件 | Blue Ice |
存放说明 | Ambient |
纯度 | >98 % |
计算分子量 | 495.48 |
分子式 | C25H34N4O2.2HCl |
可溶性/溶解性 | Soluble to 25 mM in water and to 100 mM in DMSO |
参考文献 | Adinolfiet al (2012) Expression of P2X7 receptor increases in vivo tumor growth. Cancer Res. 72 2957. PMID: 22505653. Michelet al (2008) Negative and positive allosteric modulators of the P2X7 receptor. Br.J.Pharmacol. 153 737. PMID: 18071294. Michelet al (2007) Direct labelling of the human P2X7 receptor and identification of positive and negative cooperativity of binding. Br.J.Pharmacol. 151 103. PMID: 17339830. Michel and Fonfria (2007) Agonist potency at P2X7 receptors is modulated by structurally diverse lipids. Br.J.Pharmacol. 152 523. PMID: 17700717. |