N-(4-甲氧苯基)-1-苯基-1H-吡唑-3-胺
- CAS号:103141-09-9
- 英文名:FPL 62064
- 中文名:N-(4-甲氧苯基)-1-苯基-1H-吡唑-3-胺
- CBNumber:CB51384847
- 分子式:C16H15N3O
- 分子量:265.31
- MOL File:103141-09-9.mol
- 沸点 :442.6±25.0 °C(Predicted)
- 密度 :1.15±0.1 g/cm3(Predicted)
- 储存条件 :Keep in dark place,Sealed in dry,Room Temperature
- 溶解度 :DMSO: 250 mg/mL (942.29 mM)
- 酸度系数(pKa) :2.42±0.50(Predicted)
- 形态 :Solid
- 颜色 :Light yellow to yellow
N-(4-甲氧苯基)-1-苯基-1H-吡唑-3-胺性质、用途与生产工艺
- 生物活性 FPL 62064 是一种 5-lipoxygenase (5-LOX) 和 prostaglandin synthetase (cyclooxygenase, COX) 的有效双重抑制剂,对RBL-1胞质5-LOX和精囊prostaglandin synthetase的IC50值分别为3.5 μM和3.1 μM。FPL 62064 具有有效的抗炎活性。
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靶点
Target Value seminal vesicle prostaglandin synthetase
(Cell-free assay)3.1 μM RBL-1 cytosolic 5-LOX
(Cell-free assay)3.5 μM -
体外研究
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.
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体内研究
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.
- 更新日期:2024/11/08
- 产品编号:HY-105024
- 产品名称:FPL 62064
- CAS编号:
- 包装:1 mg
- 价格:571元
- 更新日期:2024/11/08
- 产品编号:HY-105024
- 产品名称:N-(4-甲氧苯基)-1-苯基-1H-吡唑-3-胺 FPL 62064
- CAS编号:103141-09-9
- 包装:5mg
- 价格:1500元
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