PF-04745637

• 常用名: PF-04745637
• 英文名: PF-04745637
• CAS号: 1917294-46-2
• 分子量: 509.0033896
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₇H₃₂ClF₃N₂O₂
• 熔点: N/A
• 闪点: N/A

PF-04745637用途

PF-04745637 是一种有效的选择性 TRPA1 拮抗剂,对人 TRPA1 的 IC50 为 17 nM。

PF-04745637名称

• 英文名: 1-(4-chlorophenyl)-N-(2-(4-hydroxy-4-(trifluoromethyl)piperidin-1-yl)-3-phenylpropyl)cyclopentanecarboxamide

PF-04745637生物活性

• 描述: PF-04745637 是一种有效的选择性 TRPA1 拮抗剂,对人 TRPA1 的 IC50 为 17 nM。
• 相关类别:
  信号通路 >> 跨膜转运 >> TRP频道
  研究领域 >> 炎症/免疫
• 靶点实验:

  TRPA1:17 nM (IC50)

• 体内研究: 局部应用PF-04745637(化合物8；50 mg/mL和100 mg/mL)可显著降低肉桂醛介导的大鼠皮肤红肿[1]。
• 参考文献:

  [1]. Laurie B. Schenkel, et al. The discovery of a potent series of carboxamide TRPA1 antagonists. J. Med. Chem. 2016, 59, 6, 2794-2809.

PF-04745637物理化学性质

• 分子式: C₂₇H₃₂ClF₃N₂O₂
• 分子量: 509.0033896

PF-04745637靶点实验

查看更多实验

实验名称：Inhibition of cinnamaldehyde-activated full length human TRPA1 channel expressed in 2... 来源：ChEMBL 靶标：Transient receptor potential cation channel subfamily A member 1 External Id：CHEMBL3858029

实验名称：Antagonist activity at full length human TRPA1 at holding potential of 15 mV measured... 来源：ChEMBL 靶标：Transient receptor potential cation channel subfamily A member 1 External Id：CHEMBL4190659

实验名称：Stability in human liver microsomes assessed as metabolic turnover number at 10 uM af... 来源：ChEMBL 靶标：N/A External Id：CHEMBL4190622

实验名称：Passive permeability of the compound in RRCK cells 来源：ChEMBL 靶标：N/A External Id：CHEMBL4190623

实验名称：Antagonist activity at full length human TRPA1 oS5 chimera containing (870 to 896 res... 来源：ChEMBL 靶标：Transient receptor potential cation channel subfamily A member 1 External Id：CHEMBL4190624

实验名称：Suppression of cinnamaldehyde-induced flare response in Sprague-Dawley rat skin at 50... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL4190667

实验名称：Suppression of cinnamaldehyde-induced flare response in Sprague-Dawley rat skin at 50... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL4190668

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PF-04745637英文别名

• PF-04745637