中文名 | A-740003 |
英文名 | Benzeneacetamide, N-[1-[[(cyanoamino)(5-quinolinylimino)methyl]amino]-2,2-dimethylpropyl]-3,4-dimethoxy- |
别名 | 化合物A 740003 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 |
英文别名 | A 740003 A-740003 (E)-N-(1-((Cyanamido(quinolin-5-ylamino)methylene)amino)-2,2-dimethylpropyl)-2-(3,4-dimethoxyp N-[1-[[(Cyanoamino)(5-quinolinylimino)methyl]amino]-2,2-dimethylpropyl]-3,4-dimethoxybenzeneacetamide N-[1-[[(Cyanoamino)(5-quinolinylamino)methylene]amino]-2,2-dimethylpropyl]-3,4-dimethoxybenzeneacetamide Benzeneacetamide, N-[1-[[(cyanoamino)(5-quinolinylimino)methyl]amino]-2,2-dimethylpropyl]-3,4-dimethoxy- N-(1-{[(cyanoimino)(5-quinolinylamino) methyl] amino}-2,2-dimethylpropyl)-2-(3,4-dimethoxyphenyl)acetamide Benzeneacetamide, N-[1-[[(cyanoamino)(5-quinolinylamino)methylene]amino]-2,2-dimethylpropyl]-3,4-dimethoxy- 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 |
CAS | 861393-28-4 |
化学式 | C26H30N6O3 |
分子量 | 474.55 |
密度 | 1.19±0.1 g/cm3(Predicted) |
熔点 | 128-129 °C |
溶解度 | DMSO: 溶解10mg/mL,澄清 (温热) |
酸度系数 | 14.09±0.46(Predicted) |
存储条件 | 2-8°C |
外观 | 粉末 |
颜色 | white to light brown |
MDL号 | MFCD09970333 |
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. |
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. |
危险品标志 | T - 有毒物品 |
风险术语 | 25 - 吞食有毒。 |
安全术语 | 45 - 若发生事故或感不适,立即就医(可能的话,出示其标签)。 |
危险品运输编号 | UN 2811 6.1 / PGIII |
WGK Germany | 3 |
上游原料 | N-氰基-N'-5-喹啉胍 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.107 ml | 10.536 ml | 21.073 ml |
5 mM | 0.421 ml | 2.107 ml | 4.215 ml |
10 mM | 0.211 ml | 1.054 ml | 2.107 ml |
5 mM | 0.042 ml | 0.211 ml | 0.421 ml |
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