1181083-81-7
中文名称
2{[(5Z)2(1,2diazinan1yl)4oxo4,5dihydro1,3thiazol5ylidene]Methyl}5fluorophenyl pyrrolidine1carboxylate
英文名称
2{[(5Z)2(1,2diazinan1yl)4oxo4,5dihydro1,3thiazol5ylidene]Methyl}5fluorophenyl pyrrolidine1carboxylate
CAS
1181083-81-7
分子式
C19H21FN4O3S
分子量
404.46
MOL 文件
1181083-81-7.mol
更新日期
2025/05/12 15:50:30
1181083-81-7 结构式
基本信息
中文别名
化合物CLP-290 英文别名
CLP-290CLP 290
CLP290
[5-Fluoro-2-[(Z)-(2-hexahydropyridazin-1-yl-4-oxo-thiazol-5-ylidene)methyl]phenyl] pyrrolidine
2-([(5Z)-2-(1,2-DIAZINAN-1-YL)-4-OXO-4,5-DIHYDRO-1,3-THIAZOL-5-YLIDENE]METHYL)-5-FLUOROPHENYL PYRROL
2{[(5Z)2(1,2diazinan1yl)4oxo4,5dihydro1,3thiazol5ylidene]Methyl}5fluorophenyl pyrrolidine1carboxylate
(Z)-5-Fluoro-2-((4-oxo-2-(tetrahydropyridazin-1(2H)-yl)thiazol-5(4H)-ylidene)methyl)phenyl pyrrolidine-1-carboxylate
1-Pyrrolidinecarboxylic acid, 5-fluoro-2-[(Z)-[4-oxo-2-(tetrahydro-1(2H)-pyridazinyl)-5(4H)-thiazolylidene]methyl]phenyl ester
所属类别
生物化工：激动剂抑制剂物理化学性质
沸点553.7±60.0 °C(Predicted)
密度1.47±0.1 g/cm3(Predicted)
储存条件2-8°C(protect from light)
储存条件Keep in dark place,Sealed in dry,2-8°C
溶解度DMSO:23.74(Max Conc. mg/mL);58.7(Max Conc. mM)
DMSO:PBS (pH 7.2) (1:6):1.0(Max Conc. mg/mL);2.47(Max Conc. mM)
DMF:1.0(Max Conc. mg/mL);2.47(Max Conc. mM)
Ethanol:2.02(Max Conc. mg/mL);4.99(Max Conc. mM)
DMSO:PBS (pH 7.2) (1:6):1.0(Max Conc. mg/mL);2.47(Max Conc. mM)
DMF:1.0(Max Conc. mg/mL);2.47(Max Conc. mM)
Ethanol:2.02(Max Conc. mg/mL);4.99(Max Conc. mM)
酸度系数(pKa)1.29±0.20(Predicted)
形态结晶固体
颜色Off-white to yellow
常见问题列表
生物活性
CLP290 是一种神经特异性 K+-Cl− 共转运体 KCC2 的口服激活剂，具有研究多种神经和精神疾病的潜力。CLP290 能显著降低 STZ 大鼠的血液中 AVP 和血糖水平。靶点
KCC2
体内研究
CLP290 (oral gavage; 100 mg/kg; twice a day; 7 day) enhances KCC2 activity and restores Cl - transport in superficial dorsal horn (SDH) neurons of morphine-treated rats, and prevents morphine-induced hyperalgesia (MIH) in rat.
| Animal Model: | Adult male rats (300 g, >postnatal day 60) |
| Dosage: | 100 mg/kg |
| Administration: | Oral gavage; 100 mg/kg; twice a day; 7day |
| Result: | Rescued established MIH and prevented its development by restoring Cl - transport or preventing its deficiency in the SDH. |