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861393-28-4

中文名稱 N-[1-[[(氰基氨基)(5-喹啉亞氨基)甲基]氨基]-2,2-二甲基丙基]-3,4-二甲氧基苯乙酰胺
英文名稱 A-740003
CAS 861393-28-4
分子式 C26H30N6O3
分子量 474.55
MOL 文件 861393-28-4.mol
更新日期 2024/11/15 18:20:30
861393-28-4 結(jié)構(gòu)式 861393-28-4 結(jié)構(gòu)式

基本信息

中文別名
化合物A 740003
N-[1-[[(氰基氨基)(5-喹啉亞氨基)甲基]氨基]-2,2-二甲基丙基]-3,4-二甲氧基苯乙酰胺
英文別名
CS-451
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
所屬類別
生物化工:激動劑抑制劑

物理化學(xué)性質(zhì)

熔點128-129 °C
密度1.19±0.1 g/cm3(Predicted)
儲存條件2-8°C
溶解度DMSO:可溶,10mg/mL,澄清(加熱)
酸度系數(shù)(pKa)14.09±0.46(Predicted)
形態(tài)粉末
顏色白色至淺棕色

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS06
警示詞危險
危險性描述H301
防范說明P301+P310
危險品標(biāo)志T
危險類別碼25
安全說明45
危險品運輸編號UN 2811 6.1 / PGIII
WGK Germany3

常見問題列表

生物活性
A-740003 是一種有效的、選擇性的 P2X7 receptor 的競爭性拮抗劑,對大鼠和人的P2X7受體的IC50值分別為18 nM和40 nM。A-740003 可在分化的人THP-1細(xì)胞中有效地阻斷激動劑誘發(fā)的 IL-1β 釋放和孔形成,對應(yīng)的IC50值分別為156 nM和92 nM。
靶點
TargetValue
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
體外研究

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.

體內(nèi)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.

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