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1181083-81-7

中文名稱 2{[(5Z)2(1,2diazinan1yl)4oxo4,5dihydro1,3thiazol5ylidene]Methyl}5fluorophenyl pyrrolidine1carboxylate
英文名稱 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 2024/10/28 15:49:03
1181083-81-7 結(jié)構(gòu)式 1181083-81-7 結(jié)構(gòu)式

基本信息

中文別名
化合物CLP-290
英文別名
CLP-290
CLP 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
所屬類別
生物化工:激動劑抑制劑

物理化學(xué)性質(zhì)

沸點(diǎn)553.7±60.0 °C(Predicted)
密度1.47±0.1 g/cm3(Predicted)
儲存條件2-8°C(protect from light)
儲存條件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)
酸度系數(shù)(pKa)1.29±0.20(Predicted)
形態(tài)結(jié)晶固體
顏色Off-white to yellow

常見問題列表

生物活性
CLP290 是一種神經(jīng)特異性 K+-Cl? 共轉(zhuǎn)運(yùn)體 KCC2 的口服激活劑,具有研究多種神經(jīng)和精神疾病的潛力。CLP290 能顯著降低 STZ 大鼠的血液中 AVP 和血糖水平。
靶點(diǎn)

KCC2

體內(nèi)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.
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