TRPV4 antagonist 4

Names

[ Name ]:
TRPV4 antagonist 4

Biological Activity

[Description]:

TRPV4 antagonist 4 is a potent TRPV4 antagonist with an IC50 value of 22.65 nM. TRPV4 antagonist 4 inhibits TRPV4 current. TRPV4 antagonist 4 shows protective effects on acute lung injury[1].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> TRP Channel

Research Areas >> Neurological Disease

[Target]

TRPV4:22.65 nM (IC50)

[In Vitro]

TRPV4 antagonist 4 (compound 2b; 1 µM) 抑制 TRPV4-CHO 细胞中 GSK1016790A (HY-19608) (100 nM) 诱导的 TRPV4 全细胞电流[1]。 TRPV4 antagonist 4 抑制 HUVEC 中对 LPS (HY-D1056) 诱导的通透性反应[1]。

[In Vivo]

TRPV4 antagonist 4 (1 mg/kg; i.p.) 在 LPS 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]。 Animal Model: Mice (acute lung injury (ALI))[1] Dosage: 1 mg/kg Administration: I,p.; before LPS inhalation Result: Displayed significant effects to reduce the lung W/D ratio and significantly decreased the concentrations of BALF protein, significantly blocked the permeability response to LPS stimulates, greatly improved the pneumonedema, the lung pathologic changes in LPS-induced mouse lung injury mode.

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₈H₃₂Cl₂N₆O

[ Molecular Weight ]:
539.50

Related Compounds

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