Inhibitors?Screening Libraries?ProteinsMedChemExpressTRPV4 antagonist
4Cat. No.:HY-149823CAS No.:2918803-89-9分子式:C??H??Cl?N?O分子量:539.5作
用靶点:TRP Channel作用通路:Membrane Transporter/Ion Channel; Neuronal Si
gnaling储存方式:Please store the product under the recommended condit
ions inthe Certificate of Analysis.BIOLOGICAL ACTIVITY生物活性TRPV4 a
ntagonist 4 是一种有效的 TRPV4 拮抗剂，IC50 值为 22.65 nM。TRPV4 antagonist 4
抑制 TRPV4 电流。TRPV4 antagonist 4 显示出对急性肺损伤的保护作用 [1]。IC50 & TargetTR
PV422.65 nM (IC50)体外研究TRPV4 antagonist 4 (compound 2b; 1 μM) inhi
bits GSK1016790A (HY-19608) (100 nM)-induced TRPV4whole-cell curr
ents in TRPV4-CHO cells [1].TRPV4 antagonist 4 suppresses the per
meability response to LPS (HY-D1056) in HUVEC [1].体内研究TRPV4 antag
onist 4 (1 mg/kg; i.p.) improves the pneumonedema, the lung patho
logic changes in LPS-induced mouse lung injury mode [1].Animal Mo
del:Mice (acute lung injury (ALI)) [1]Dosage:1 mg/kgAdministratio
n:I,p.; before LPS inhalationResult:Displayed significant effects
to reduce the lung W/D ratio and significantly decreased theconc
entrations of BALF protein, significantly blocked the permeabilit
y response to LPSstimulates, greatly improved the pneumonedema, t
he lung pathologic changes in LPS-induced mouse lung injury mode.
1/2Master of Bioactive Molecules — 您身边的抑制剂大师MedChemExpressREFEREN
CESAi C, et al. Discovery and pharmacological characterization of
a novel benzimidazole TRPV4 antagonist with cyanocyclobutyl moie
ty. Eur J Med Chem. 2023 Mar 5;249:115137.McePdfHeightCaution: Pr
oduct has not been fully validated for medical applications.For r
esearch use only.2/2Master of Bioactive Molecules — 您身边的抑制剂大师 |
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