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103141-09-9

中文名稱 N-(4-甲氧苯基)-1-苯基-1H-吡唑-3-胺
英文名稱 FPL 62064
CAS 103141-09-9
分子式 C16H15N3O
分子量 265.31
MOL 文件 103141-09-9.mol
更新日期 2024/12/15 19:35:20
103141-09-9 結(jié)構(gòu)式 103141-09-9 結(jié)構(gòu)式

基本信息

中文別名
N-(4-甲氧苯基)-1-苯基-1H-吡唑-3-胺
英文別名
FPL 62064
N-(4-Methoxyphenyl)-1-phenyl-1H-pyrazol-3-amine
1H-Pyrazol-3-amine,N-(4-methoxyphenyl)-1-phenyl-

物理化學(xué)性質(zhì)

沸點(diǎn)442.6±25.0 °C(Predicted)
密度1.15±0.1 g/cm3(Predicted)
儲(chǔ)存條件Keep in dark place,Sealed in dry,Room Temperature
溶解度DMSO: 250 mg/mL (942.29 mM)
酸度系數(shù)(pKa)2.42±0.50(Predicted)
形態(tài)Solid
顏色Light yellow to yellow

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS08
警示詞警告
危險(xiǎn)性描述H341

常見(jiàn)問(wèn)題列表

生物活性
FPL 62064 是一種 5-lipoxygenase (5-LOX) 和 prostaglandin synthetase (cyclooxygenase, COX) 的有效雙重抑制劑，對(duì)RBL-1胞質(zhì)5-LOX和精囊prostaglandin synthetase的IC50值分別為3.5 μM和3.1 μM。FPL 62064 具有有效的抗炎活性。
靶點(diǎn)
TargetValue
seminal vesicle prostaglandin synthetase
(Cell-free assay) 		3.1 μM
RBL-1 cytosolic 5-LOX
(Cell-free assay) 		3.5 μM
體外研究

FPL 62064 inhibits both 5-1ipoxygenase (IC 50 of 3.5 μM for RBL-1 cytosolic 5-1ipoxygenase) and prostaglandin synthetase (IC 50 of 3.1 μM for seminal vesicle prostaglandin synthetase ) with equal facility in the isolated enzyme screens. However in the intact RBL-I cell prostaglandin synthetase (IC 50 of 3.6 μM) is more readily inhibited by FPL 62064 than is 5-1ipoxygenase (IC 50 of 31 μM). This difference in sensitivity is not reflected in the mouse macrophage where the IC 50 s for leukotriene (IC 50 of 0.72 μM) and prostaglandin (IC 50 of 0.43 μM) production are similar.

體內(nèi)研究

FPL 62064 (5-20 mg/kg; intraperitoneal injection; female LACA mice) treatment inhibits peritoneal inflammation induced by immune-complex.

Animal Model: Female LACA mice (20-30 g) injected with immune complex.
Dosage: 5 mg/kg, 10 mg/kg, 20 mg/kg
Administration: Intraperitoneal injection
Result: Produced a dose-related inhibition of dye extravasation, leukotriene C 4 (LTC 4 ) and prostaglandin E 2 (PGE 2 ) formation.
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