CID 16020046 是一种选择性 GPR55 拮抗剂,在酵母中抑制 GPR55 组成型活性,IC50 为 0.15 μM。它抑制 GPR55 介导的 Ca2+信号传导和 GPR55 介导的 ERK1/2 磷酸化,可降低内皮细胞的伤口愈合,参与血小板功能的调节。
产品描述
CID16020046 is a selective GPR55 antagonist, inhibiting GPR55 constitutive activity with IC50 of 0.15 μM in yeast.
体外活性
In yeast cells expressing human GPR55, CID16020046 inhibited agonist-induced receptor activation. In human embryonic kidney (HEK293) cells stably expressing human GPR55, CID16020046 behaved as an antagonist on LPI-mediated Ca2+ release and extracellular signal-regulated kinases activation, but not in HEK293 cells expressing cannabinoid receptor 1 or 2 (CB1 or CB2). CID16020046 dose-dependently inhibited lysophosphatidylinositol (LPI)-induced activation of nuclear factor of activated T-cells (NFAT), nuclear factor κ of activated B cells (NF-κB) and serum response element, translocation of NFAT and NF-κB, and GPR55 internalization [1].
Cas No.
834903-43-4
分子式
C25H19N3O4
分子量
425.444
别名
C390-0219
储存和溶解度
DMSO:40 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years