N-[1-[[(氰基氨基)(5-喹啉亚氨基)甲基]氨基]-2,2-二甲基丙基]-3,4-二甲氧基苯乙酰胺
- CAS号:861393-28-4
- 英文名:A-740003
- 中文名:N-[1-[[(氰基氨基)(5-喹啉亚氨基)甲基]氨基]-2,2-二甲基丙基]-3,4-二甲氧基苯乙酰胺
- CBNumber:CB61871931
- 分子式:C26H30N6O3
- 分子量:474.55
- MOL File:861393-28-4.mol
- 熔点 :128-129 °C
- 密度 :1.19±0.1 g/cm3(Predicted)
- 储存条件 :2-8°C
- 溶解度 :DMSO: soluble10mg/mL, clear (warmed)
- 酸度系数(pKa) :14.09±0.46(Predicted)
- 形态 :powder
- 颜色 :white to light brown
N-[1-[[(氰基氨基)(5-喹啉亚氨基)甲基]氨基]-2,2-二甲基丙基]-3,4-二甲氧基苯乙酰胺性质、用途与生产工艺
- 生物活性 A-740003 是一种有效的、选择性的 P2X7 receptor 的竞争性拮抗剂,对大鼠和人的P2X7受体的IC50值分别为18 nM和40 nM。A-740003 可在分化的人THP-1细胞中有效地阻断激动剂诱发的 IL-1β 释放和孔形成,对应的IC50值分别为156 nM和92 nM。
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靶点
Target Value rat P2X7 receptor
(Cell-free assay)18 nM human P2X7 receptor
(Cell-free assay)40 nM IL-1β pore formation
(Cell-based assay)92 nM IL-1β release
(Cell-based assay)156 nM -
体外研究
A 438079 or A 740003 (10 μM) significantly blocks the sustained phase of the BzATP-induced response. A-740003 infusion reduces SE-induced TNF-α expression in dentate granule cells. A-740003 infusions increases SE-induced neuronal death. 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. A-740003 potently blocks agonist-evoked IL-1β release with (IC 50 =156 nM) and pore formation (IC 50 =92 nM) in differentiated human THP-1 cells.
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体内研究
Systemic administration of A-740003 produces dose-dependent antinociception in a spinal nerve ligation model (ED 50 =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 (ED 50 =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.
- 更新日期:2024/08/19
- 产品编号:HY-50697
- 产品名称:A-740003
- CAS编号:
- 包装:5 mg
- 价格:425元
- 更新日期:2024/08/19
- 产品编号:HY-50697
- 产品名称:N-[1-[[(氰基氨基)(5-喹啉亚氨基)甲基]氨基]-2,2-二甲基丙基]-3,4-二甲氧基苯乙酰胺 A-740003
- CAS编号:861393-28-4
- 包装:10mg
- 价格:680元
- 公司名称:TOCRIS-US
- 联系电话:--
- 电子邮件:customerservice@tocris.co.uk
- 国家:英国
- 产品数:5729
- 优势度:77