CID 16020046 |
| Catalog No.GC35694 |
Le CID 16020046 est un antagoniste puissant et sélectif du GPR55 et inhibe l'activité constitutive du GPR55 avec une IC50 de 0,15 μM. Le CID 16020046 inhibe la signalisation Ca2+ médiée par GPR55 et la phosphorylation ERK1/2 médiée par GPR55. Le CID 16020046 réduit la cicatrisation des plaies dans les cellules endothéliales et est impliqué dans la régulation de la fonction plaquettaire.
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Cas No.: 834903-43-4
Sample solution is provided at 25 µL, 10mM.
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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.
[1]. Kargl J, et al. A selective antagonist reveals a potential role of G protein-coupled receptor 55 in platelet and endothelial cell function. J Pharmacol Exp Ther. 2013 Jul;346(1):54-66.
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