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编 号:F756844
分子式:C28H32Cl2N6O
分子量:539.5
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生物活性:
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.

体内研究:
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。Animal Model:Mice (acute lung injury (ALI))
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.

体外研究:
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。TRPV4 antagonist 4 抑制 HUVEC 中对 LPS (HY-D1056) 诱导的通透性反应。
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