TRPV4 antagonist 4

• 常用名: TRPV4 antagonist 4
• 英文名: TRPV4 antagonist 4
• CAS号: 2918803-89-9
• 分子量: 539.50
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₈H₃₂Cl₂N₆O
• 熔点: N/A
• 闪点: N/A

TRPV4 antagonist 4用途

TRPV4拮抗剂4是一种有效的TRPV4阻断剂,其IC50值为22.65nM。TRPV4拮抗剂4抑制TRPV4电流。TRPV4拮抗剂4对急性肺损伤具有保护作用[1]。

TRPV4 antagonist 4名称

• 英文名: TRPV4 antagonist 4

TRPV4 antagonist 4生物活性

• 描述: TRPV4拮抗剂4是一种有效的TRPV4阻断剂,其IC50值为22.65nM。TRPV4拮抗剂4抑制TRPV4电流。TRPV4拮抗剂4对急性肺损伤具有保护作用[1]。
• 相关类别:
  信号通路 >> 跨膜转运 >> TRP频道
  研究领域 >> 神经疾病
• 靶点实验:

  TRPV4:22.65 nM (IC50)

• 体外研究: TRPV4拮抗剂4(化合物2b；1µM)抑制 TRPV4-槽细胞中 GSK1016790A(HY-19608)(100 nM)诱导的 TRPV4型全细胞电流[1] TRPV4拮抗剂4抑制 胡维克中对 脂多糖(HY-D1056)诱导的通透性反应[1]
• 体内研究: TRPV4拮抗剂4(1 mg/kg；腹腔注射)在 脂多糖诱导的小鼠肺损伤模式中改善肺水肿和相关肺病理变化[1] 动物模型：小鼠(急性肺损伤)[1]剂量：1 mg/kg给药：I,p。；结果：显示出显著降低肺W/D比和显著降低BALF蛋白浓度的作用,显著阻断LPS刺激下的通透性反应,显著改善LPS诱导的小鼠肺损伤模式下的肺水肿、肺病理改变。
• 参考文献:

  [1]. Ai C, et al. Discovery and pharmacological characterization of a novel benzimidazole TRPV4 antagonist with cyanocyclobutyl moiety. Eur J Med Chem. 2023 Mar 5;249:115137.

TRPV4 antagonist 4物理化学性质

• 分子式: C₂₈H₃₂Cl₂N₆O
• 分子量: 539.50
• InChIKey: HKOYZUBWZOWYKY-UHFFFAOYSA-N
• SMILES: CC(=O)Nc1c(Cl)c(Cl)cc2c1nc(NC(C)C)n2C1CCN(c2ccc(C3(C#N)CCC3)cc2)CC1

TRPV4 antagonist 4靶点实验

查看更多实验

实验名称：Antiinflammatory activity in LPS-induced acute lung injury mouse model assessed as BA... 来源：ChEMBL 靶标：Mus musculus External Id：CHEMBL5347923

实验名称：Antiinflammatory activity in LPS-induced acute lung injury mouse model assessed as pa... 来源：ChEMBL 靶标：Mus musculus External Id：CHEMBL5347924

实验名称：Inhibition of LPS-induced hyper-permeability in human HUVEC cells assessed as reducti... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5347921

实验名称：Antiinflammatory activity in LPS-induced acute lung injury mouse model assessed as re... 来源：ChEMBL 靶标：Mus musculus External Id：CHEMBL5347922

实验名称：Antagonist activity at TRPV4 (unknown origin) expressed in CHO cells assessed as inhi... 来源：ChEMBL 靶标：Transient receptor potential cation channel subfamily V member 4 External Id：CHEMBL5347919

实验名称：Antagonist activity at TRPV4 (unknown origin) expressed in CHO cells assessed as inhi... 来源：ChEMBL 靶标：Transient receptor potential cation channel subfamily V member 4 External Id：CHEMBL5347917

实验名称：Antagonist activity at TRPV4 (unknown origin) expressed in CHO cells assessed as inhi... 来源：ChEMBL 靶标：Transient receptor potential cation channel subfamily V member 4 External Id：CHEMBL5347918

实验名称：Potency index, ratio of HC-067047 IC50 to test compound IC50 for antagonist activity ... 来源：ChEMBL 靶标：Transient receptor potential cation channel subfamily V member 4 External Id：CHEMBL5347915

实验名称：Antagonist activity at TRPV4 (unknown origin) assessed as inhibition of capsaicin ind... 来源：ChEMBL 靶标：Transient receptor potential cation channel subfamily V member 4 External Id：CHEMBL5347916

实验名称：Antagonist activity at TRPV4 (unknown origin) expressed in Flp-In-CHO cells assessed ... 来源：ChEMBL 靶标：Transient receptor potential cation channel subfamily V member 4 External Id：CHEMBL5347913

共12条，当前第1页，共2页

1

2