1125758-85-1
中文名称
1-CYANO-2-[(1S)-1-PHENYLETHYL]-3-QUINOLIN-5-YLGUANIDINE
英文名称
A 804598
CAS
1125758-85-1
分子式
C19H17N5
分子量
315.37
MOL 文件
1125758-85-1.mol
更新日期
2024/05/07 11:49:58
1125758-85-1 结构式
基本信息
中文别名
化合物CZC25146A-804598游离态
英文别名
CS-2234A 804598
A-804598 （(A 804598
1-cyano-2-[(1S)-1-phenylethyl]-3-quinolin-5-ylguanidine
2-Cyano-1-[(1S)-1-phenylethyl]-3-(5-quinolinyl)guanidine
N-Cyano-N′′-[(1S)-1-phenylethyl]-N′-5-quinolinyl-guanidine
Guanidine, N-cyano-N''-[(1S)-1-phenylethyl]-N'-5-quinolinyl-
所属类别
生物化工：激动剂抑制剂物理化学性质
沸点498.0±47.0 °C(Predicted)
密度1.17±0.1 g/cm3(Predicted)
储存条件Keep in dark place,Sealed in dry,2-8°C
溶解度DMSO：可溶10mg/mL，澄清
酸度系数(pKa)4.52±0.12(Predicted)
形态粉末
颜色白色至米色
常见问题列表
生物活性
A-804598 是一个 CNS 渗透，竞争性和选择性的 P2X7 受体拮抗剂，作用于小鼠，大鼠和人的 P2X7 受体，IC50s 分别是 9 nM, 10 nM 和 11 nM。靶点
IC50: 9 nM (mouse P2X7 receptor), 10 nM (rat P2X7 receptor), 11 nM (human P2X7 receptor)
体外研究
Pre-incubation with A-804598 (0.1-10 μM; 1 hour) significantly attenuates BzATP-induced cell loss in a concentration-dependent manner. 3 μM A-804598 exhibits the greatest protective effect against BzATP-induced cytotoxicity.
Cell Cytotoxicity Assay
| Cell Line: | microglial cell |
| Concentration: | 0.1, 0.3, 1, 3, 10 μM |
| Incubation Time: | 1 hour |
| Result: | Protected against BzATP-induced cytotoxicity in both inactivated and activated microglia. |
体内研究
A chroni treatment with A-804598 (intraperitoneal injection; 30 mg/kg; five times a week) decreases the expression of LC3B-II and SQSTM1/p62 in lumbar spinal cord at end stage of disease.
| Animal Model: | Adult B6.Cg-Tg (SOD1-G93A) 1Gur/J female mice |
| Dosage: | 30 mg/kg |
| Administration: | Intraperitoneal injection; five times a week |
| Result: | Decreased SQSTM1/p62 expression. |