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
中文名称 | 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 |
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中文同义词 | 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;化合物A 740003 |
英文名称 | A-740003 |
英文同义词 | N-[1-[[(Cyanoamino)(5-quinolinylamino)methylene]amino]-2,2-dimethylpropyl]-3,4-dimethoxybenzeneacetamide;A-740003 N-[1-[[(Cyanoamino)(5-quinolinylimino)methyl]amino]-2,2-dimethylpropyl]-3,4-dimethoxybenzeneacetamide;N-[1-[[(Cyanoamino)(5-quinolinylimino)methyl]amino]-2,2-dimethylpropyl]-3,4-dimethoxybenzeneacetamide A-740003;N-(1-{[(cyanoimino)(5-quinolinylamino) methyl] amino}-2,2-dimethylpropyl)-2-(3,4-dimethoxyphenyl)acetamide;A-740003, >=99%;(E)-N-(1-((Cyanamido(quinolin-5-ylamino)methylene)amino)-2,2-dimethylpropyl)-2-(3,4-dimethoxyp;A-740003;N-[1-[[(Cyanoamino)(5-quinolinylimino)methyl]amino]-2,2-dimethylpropyl]-3,4-dimethoxybenzeneacetamide |
CAS号 | 861393-28-4 |
分子式 | C26H30N6O3 |
分子量 | 474.55 |
EINECS号 | |
相关类别 | |
Mol文件 | 861393-28-4.mol |
结构式 | ![]() |
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
熔点 | 128-129 °C |
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密度 | 1.19±0.1 g/cm3(Predicted) |
储存条件 | 2-8°C |
溶解度 | DMSO:可溶,10mg/mL,澄清(加热) |
酸度系数(pKa) | 14.09±0.46(Predicted) |
形态 | 粉末 |
颜色 | 白色至浅棕色 |
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 |
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.
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 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/04/30 | HY-50697 | A-740003 | 5 mg | 425元 | |
2024/04/30 | HY-50697 | 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 | 861393-28-4 | 10mM * 1mLin DMSO | 748元 |