1-CYANO-2-[(1S)-1-PHENYLETHYL]-3-QUINOLIN-5-YLGUANIDINE
| 中文名称 | 1-CYANO-2-[(1S)-1-PHENYLETHYL]-3-QUINOLIN-5-YLGUANIDINE |
|---|---|
| 中文同义词 | A-804598游离态;化合物CZC25146;S-2-氰基-1-(1-苯乙基)-3-(喹啉-5-基)胍;A 804598,P2X7拮抗剂 |
| 英文名称 | A 804598 |
| 英文同义词 | A 804598;N-Cyano-N′′-[(1S)-1-phenylethyl]-N′-5-quinolinyl-guanidine;1-cyano-2-[(1S)-1-phenylethyl]-3-quinolin-5-ylguanidine;2-Cyano-1-[(1S)-1-phenylethyl]-3-(5-quinolinyl)guanidine;A-804598 （(A 804598;CS-2234;Guanidine, N-cyano-N''-[(1S)-1-phenylethyl]-N'-5-quinolinyl-;S-2-Cyano-1-(1-phenylethyl)-3-(quinolin-5-yl)guanidine |
| CAS号 | 1125758-85-1 |
| 分子式 | C19H17N5 |
| 分子量 | 315.37 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 1125758-85-1.mol |
| 结构式 | ![1-CYANO-2-[(1S)-1-PHENYLETHYL]-3-QUINOLIN-5-YLGUANIDINE 结构式](CAS/20180713/GIF/1125758-85-1.gif) |
1-CYANO-2-[(1S)-1-PHENYLETHYL]-3-QUINOLIN-5-YLGUANIDINE 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 |
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。
IC50: 9 nM (mouse P2X7 receptor), 10 nM (rat P2X7 receptor), 11 nM (human P2X7 receptor)
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. |
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. |
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-100483 | A-804598 | 1 mg | 300元 | |
| 2024/04/30 | HY-100483 | 1-CYANO-2-[(1S)-1-PHENYLETHYL]-3-QUINOLIN-5-YLGUANIDINE A-804598 | 1125758-85-1 | 5mg | 550元 |