CID 16020046 |
| Katalog-Nr.GC35694 |
CID 16020046 ist ein potenter und selektiver GPR55-Antagonist und hemmt die konstitutive AktivitÄt von GPR55 mit einem IC50 von 0,15 μM. CID 16020046 hemmt die GPR55-vermittelte Ca2+-Signalgebung und die GPR55-vermittelte ERK1/2-Phosphorylierung. CID 16020046 reduziert die Wundheilung in Endothelzellen und ist an der Regulierung der BlutplÄttchenfunktion beteiligt.
Products are for research use only. Not for human use. We do not sell to patients.
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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