CID 16020046
Names
Biological Activity
[Description]:
CID 16020046 is a potent and selective GPR55(LPI receptor) antagonist; inhibitsGPR55 constitutive activity with IC50 of 0.15 uM.IC50 value: 0.15 uM [1]Target: GPR55 antagonistIn yeast cells expressing human GPR55, CID16020046 antagonized agonist-induced receptor activation. In human embryonic kidney(HEK293) cells stably expressing human GPR55, the compound 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.CID16020046 concentration dependently inhibited LPI-induced activation of nuclear factor of activated T-cells (NFAT), nuclear factor k of activated B cells (NF-kB) and serum response element, translocation of NFAT and NF-kB, and GPR55 internalization. It reduced LPI-induced wound healing in primary human lung microvascular endothelial cells and reversed LPI-inhibited platelet aggregation.
[Related Catalog]:
[References]
[Related Small Molecules]
Chemical & Physical Properties
[ Molecular Formula ]:
C25H19N3O4
[ Molecular Weight ]:
425.43600
[ Exact Mass ]:
425.13800
[ PSA ]:
106.52000
[ LogP ]:
4.60370
[ Storage condition ]:
-20℃
Safety Information
[ Symbol ]:
GHS07
[ Signal Word ]:
Warning
[ Hazard Statements ]:
H315-H319
[ Precautionary Statements ]:
P305 + P351 + P338
[ RIDADR ]:
NONH for all modes of transport