CID 16020046 |
| Catalog No.GC35694 |
CID 16020046은 강력하고 선택적인 GPR55 길항제이며 0.15μM의 IC50으로 GPR55 구성 활성을 억제합니다. CID 16020046은 GPR55 매개 Ca2+ 신호 전달 및 GPR55 매개 ERK1/2 인산화를 억제합니다. CID 16020046은 내피 세포의 상처 치유를 감소시키고 혈소판 기능의 조절에 관여합니다.
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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