1-CYANO-2-[(1S)-1-PHENYLETHYL]-3-QUINOLIN-5-YLGUANIDINE

生物活性靶点体外研究体内研究 1-CYANO-2-[(1S)-1-PHENYLETHYL]-3-QUINOLIN-5-YLGUANIDINE 试剂级价格

CAS号:1125758-85-1
英文名:A 804598
中文名:1-CYANO-2-[(1S)-1-PHENYLETHYL]-3-QUINOLIN-5-YLGUANIDINE
CBNumber:CB82602998
分子式:C19H17N5
分子量:315.37
MOL File:1125758-85-1.mol

1-CYANO-2-[(1S)-1-PHENYLETHYL]-3-QUINOLIN-5-YLGUANIDINE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: soluble10mg/mL, clear
酸度系数(pKa) :4.52±0.12(Predicted)
形态 :powder
颜色 :white to beige

安全信息

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

1-CYANO-2-[(1S)-1-PHENYLETHYL]-3-QUINOLIN-5-YLGUANIDINE性质、用途与生产工艺

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.