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A-740003

A-740003

产品编号 T3690   CAS 861393-28-4
别名: A 740003

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。

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A-740003 Chemical Structure
A-740003, CAS 861393-28-4
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
产品目录号及名称: A-740003 (T3690)
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纯度: 96.53%
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生物活性
化学信息
存储 & 溶解度
参考文献
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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 9.5 mg/mL(20 mM)

溶液配制表

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

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Kim, J., Ryu, H., & Kang, T. (2011). P2X7 receptor activation ameliorates CA3 neuronal damage via a tumor necrosis factor-α-mediated pathway in the rat hippocampus following status epilepticus. Journal Of Neuroinflammation, 8(1), 62. doi: 10.1186/1742-2094-8-62 2. Donnelly-Roberts DL, et al. Mammalian P2X7 receptor pharmacology: comparison of recombinant mouse, rat and human P2X7 receptors.Br J Pharmacol. 2009 Aug;157(7):1203-14. Epub 2009 Jun 22. 3. Honore P, et al. A-74202003 [N-(1-{[(cyanoimino)(5-quinolinylamino) methyl]amino}-2,2-dimethylpropyl)-2-(3,4-dimethoxyphenyl)acetamide], a novel and selective P2X7 receptor antagonist, dose-dependently reduces neuropathic pain in the rat. J Pharmacol Exp Th 4. Tian C, Han X, He L, et al. Transient receptor potential ankyrin 1 contributes to the ATP-elicited oxidative stress and inflammation in THP-1-derived macrophage[J]. Molecular and Cellular Biochemistry. 2020: 1-14.

文献引用

1. Xiao Z, Xu M, Lan L, et al. Activation of the P2X7 receptor in the dental pulp tissue contributes to the pain in rats with acute pulpitis. Molecular Pain. 2022, 18: 17448069221106844 2. Tian C, Han X, He L, et al. Transient receptor potential ankyrin 1 contributes to the ATP-elicited oxidative stress and inflammation in THP-1-derived macrophage. Molecular and Cellular Biochemistry. 2020: 1-14
A 438079 Piromelatine P2X3 antagonist 38 CE-224535 BzATP triethylammonium salt A 839977 Minodronic acid NF023 hexasodium

相关化合物库

该产品包含在如下化合物库中:
抗癌活性化合物库 神经退行性疾病化合物库 经典已知活性库 抗癌化合物库 离子通道库 NO PAINS 化合物库 神经信号分子库 已知活性化合物库 临床前化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

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。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% ddH2O
计算 重置

技术支持

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。

Keywords

A-740003 861393-28-4 Membrane transporter/Ion channel Neuroscience P2X Receptor P2XRs inhibit A 740003 Inhibitor A740003 inhibitor

 

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