Powder: -20°C for 3 years | In solvent: -80°C for 1 year
A-740003 (A 740003) 是一种选择性和竞争性的P2X7 受体拮抗剂,抑制大鼠和人的 P2X7 受体,IC50值分别为 18 和 40 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 231 | 现货 | ||
5 mg | ¥ 347 | 现货 | ||
10 mg | ¥ 558 | 现货 | ||
50 mg | ¥ 676 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 347 | 现货 |
产品描述 | A-740003 (A 740003) is an effective and specific P2X7 receptor antagonist (IC50: 18/40 nM, for rat/human). It can reduce nociception in animal models of persistent neuropathic and inflammatory pain, and also reduce neuroblastoma tumor growth in mice. |
靶点活性 | P2X7(rat):18nM, P2X7(hμMan) :40 nM |
体外活性 | A 438079 or A 740003 (10 μM) significantly blocks the sustained phase of the BzATP-induced response[1]. A-740003 infusion reduces SE-induced TNF-α expression in dentate granule cells. A-740003 infusions increases SE-induced neuronal death[2]. A-740003 and A-438079 show significantly greater potency in blocking P2X7 receptor activation across all species compared with other antagonists. A-740003 and A-438079 show greater activity at rat and human, as compared with mouse P2X7 receptors[3]. A-740003 potently blocks agonist-evoked IL-1β release with (IC50=156 nM) and pore formation (IC50=92 nM) in differentiated human THP-1 cells[4]. |
体内活性 | Systemic administration of A-740003 produces dose-dependent antinociception in a spinal nerve ligation model (ED50=19 mg/kg i.p.) in the rat. A-740003 also attenuates tactile allodynia in two other models of neuropathic pain, chronic constriction injury of the sciatic nerve and vincristine-induced neuropathy. In addition, A-740003 effectively reduces thermal hyperalgesia observed following intraplantar administration of carrageenan or complete Freund's adjuvant (ED50=38-54 mg/kg i.p.). A-740003 is ineffective in attenuating acute thermal nociception in normal rats and does not alter motor performance at analgesic doses[4]. |
别名 | A 740003 |
分子量 | 474.55 |
分子式 | C26H30N6O3 |
CAS No. | 861393-28-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 9.5 mg/mL(20 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.1073 mL | 10.5363 mL | 21.0726 mL | 52.6815 mL |
5 mM | 0.4215 mL | 2.1073 mL | 4.2145 mL | 10.5363 mL | |
10 mM | 0.2107 mL | 1.0536 mL | 2.1073 mL | 5.2681 mL | |
20 mM | 0.1054 mL | 0.5268 mL | 1.0536 mL | 2.6341 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
A-740003 861393-28-4 Membrane transporter/Ion channel Neuroscience P2X Receptor P2XRs inhibit A 740003 Inhibitor A740003 inhibitor