TRPV4 agonist-1 是一种瞬时受体电位香草酸亚型 4 (TRPV4) 激动剂,在 hTRPV4 Ca2+ 实验中 EC50 为 60nM。
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TRPV4 agonist-1 Chemical Structure
分子量:484.93
分子式:C₂₅H₂₃ClF₂N₄O₂
描述:TRPV4激动剂-1是一种瞬时受体电位香草酸4(TRPV4)激动剂,在hTRPV4 Ca2 +测定中EC50为60 nM [1]。
IC50 & Target:EC50: 60 nM (hTRPV4 hTRPV4 Ca2+)[1]
体外:TRPV4激动剂-1(化合物36)表现出显着增加的效力(在SOX9报道分子测定中ECmax:20nM)。TRPV4激动剂-1对TRPV1通道无活性[1]。
相关文献:
[1]. Atobe M, et al. Discovery of Novel Transient Receptor PotentialVanilloid 4 (TRPV4) Agonists as Regulators of Chondrogenic Differentiation:Identification of Quinazolin-4(3 H)-ones and in Vivo Studies on a SurgicallyInduced Rat Model of Osteoarthritis. J Med Chem. 2019 Jan 28.
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