CID 16020046 |
| カタログ番号GC35694 |
CID 16020046 は、強力かつ選択的な GPR55 アンタゴニストであり、0.15 μM の IC50 で GPR55 の構成的活性を阻害します。 CID 16020046 は、GPR55 を介した Ca2+ シグナル伝達と GPR55 を介した ERK1/2 リン酸化を阻害します。 CID 16020046 は、内皮細胞の創傷治癒を低下させ、血小板機能の調節に関与しています。
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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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