2918803-89-9

2918803-89-9 structure

Name: TRPV4 antagonist 4
Chemical Name: TRPV4 antagonist 4
CAS Number: 2918803-89-9
Molecular Formula: C₂₈H₃₂Cl₂N₆O
Molecular Weight: 539.50
Catalog: Signaling Pathways Membrane Transporter/Ion Channel TRP Channel
Create Date: 2023-05-31 18:39:31
Modify Date: 2024-01-09 00:51:10
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].

Name	TRPV4 antagonist 4

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.

Molecular Formula	C₂₈H₃₂Cl₂N₆O
Molecular Weight	539.50