309712-55-8
中文名稱
GW791343 HCl
英文名稱
GW791343 HCl
CAS
309712-55-8
分子式
C20H27Cl3F2N4O
分子量
483.81
MOL 文件
309712-55-8.mol
更新日期
2024/06/06 11:49:22
309712-55-8 結(jié)構(gòu)式
基本信息
中文別名
化合物GW791343 3HCL 英文別名
GW791343 3HClGW791343 HCl USP/EP/BP
GW791343 (trihydrochloride)
GW 791343 TRIHYDROCHLORIDE
GW-791343 TRIHYDROCHLORIDE
2-(3,4-difluorophenylamino)-N-(2-methyl-5-(piperazin-1-ylmethyl)phenyl)acetamide trihydrochloride
2-((3,4-difluorophenyl)amino)-N-(2-methyl-5-(piperazin-1-ylmethyl)phenyl)acetamide hydrogen chloride
所屬類別
生物化工：P2 Receptor 抑制劑物理化學(xué)性質(zhì)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度Soluble to 100 mM in water and to 100 mM in DMSO
形態(tài)粉末
CAS 數(shù)據(jù)庫309712-55-8
常見問題列表
生物活性
GW791343 HCl是GW791343的鹽酸鹽形式，是一種非競(jìng)爭(zhēng)性的人類P2X7 receptor變構(gòu)抑制劑，pIC50為7。體外研究
In cells expressing human P2X7 receptors, GW 791343 inhibits agonist-stimulated ethidium accumulation in both sucrose and NaCl buffer. In NaCl buffer, GW 791343 reduces the maximal response to both ATP and BzATP, but there is little effect on agonist potency except for a decrease in the presence of 300–1000 nM GW 791343. GW 791343 also reduces maximal responses to ATP and BzATP in sucrose buffer, although this effect is more marked when using ATP as agonist. In sucrose buffer, GW 791343 produces a slight decrease in ATP potency at 300 nM. GW 791343 decreases BzATP potency at concentrations of 300 nM to 10 μM. A more marked increase in agonist effect is observed when using ATP as agonist in NaCl buffer with GW791343 increasing the pEC50 and maximal response to ATP at concentrations of 10 and 30 μM. In sucrose buffer, GW791343 also increases responses when using ATP as agonist. GW791343 inhibits responses at the human–rat chimeric receptor in both sucrose and NaCl buffer. GW791343 increases responses to BzATP at the F95L mutant receptor. GW791343 is a non-competitive antagonist and negative allosteric modulator at the human P2X7 receptor; however, GW 791343 also acts as a positive allosteric modulator at the rat P2X7 receptor. At the dog P2X7 receptor, GW 791343 is an antagonist with similar potency to that determined at the human receptor.