861393-28-4
基本信息
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
A-740003, >=99%
A 740003
A740003
A740003 - CAS 861393-28-4 - Calbiochem
P2XRs,P2X Receptor,inhibit,A-740003,A740003,Inhibitor
(E)-N-(1-((Cyanamido(quinolin-5-ylamino)methylene)amino)-2,2-dimethylpropyl)-2-(3,4-dimethoxyp
N-(1-(3-Cyano-2-(quinolin-5-yl)guanidino)-2,2-dimethylpropyl)-2-(3,4-dimethoxyphenyl)acetamide
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
物理化学性质
| 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：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 |
安全数据
| 危险性符号(GHS) |  GHS06 |
| 警示词 | 危险 |
| 危险性描述 | H301 |
| 防范说明 | P301+P310 |
| 危险品标志 | T |
| 危险类别码 | 25 |
| 安全说明 | 45 |
| 危险品运输编号 | UN 2811 6.1 / PGIII |
| WGK Germany | 3 |
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价格(试剂级)
| 报价日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
| 2025/02/08 | 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 | 5 mg | 425元 |
| 2025/02/08 | 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 | 10mg | 680元 |
| 2025/02/08 | 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 |
常见问题列表
| 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.