同义名 :	C390-0219
	CAS号 :	834903-43-4
	货号 :	A843612
	分子式 :	C25H19N3O4
	纯度 :	99%+
	分子量 :	425.44
	MDL号 :	MFCD06196075
	存储条件：	Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	动物实验配方：

生物活性

描述

The G protein-coupled receptor 55 (GPR55), a lysophosphatidylinositol (LPI) receptor that is responsive to certain cannabinoids, has been implicated in several (patho)physiologic functions. CID-16020046 (40 nM – 10 μM) acts as an inverse agonist, inhibiting GPR55 constitutive activity with an IC50 of 0.15 μM. In HEK-GPR55 cells, pretreatment with increasing concentrations of CID-16020046 inhibited GPR55 agonist-induced intracellular Ca2+ release. Further, 2.5 μM CID-16020046 significantly inhibited the LPI (a GPR55 agonist)-induced ERK1/2 phosphorylation, GPR55 internalization and GPR55-mediated transcription factor activation in HEK-GPR55 cells[3]. In the DSS (dextran sulfate sodium) and TNBS (trinitrobenzene sulfonic acid) colitis models, treatment with CID-16020046 at a dosage of 20 mg/kg significantly reduced macroscopic scores and MPO (myeloperoxidase) activity as compared to vehicle-treated animals[4].

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	2.35mL 0.47mL 0.24mL	11.75mL 2.35mL 1.18mL	23.51mL 4.70mL 2.35mL

参考文献

[1]AlSuleimani YM, Hiley CR. The GPR55 agonist lysophosphatidylinositol relaxes rat mesenteric resistance artery and induces Ca(2+) release in rat mesenteric artery endothelial cells. Br J Pharmacol. 2015 Jun;172(12):3043-57. [2]Kargl J, Brown AJ, 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. [3]Kargl J, Brown AJ, Andersen L, Dorn G, Schicho R, Waldhoer M, Heinemann A. 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 [4]Stančić A, Jandl K, Hasenöhrl C, Reichmann F, Marsche G, Schuligoi R, Heinemann A, Storr M, Schicho R. The GPR55 antagonist CID16020046 protects against intestinal inflammation. Neurogastroenterol Motil. 2015 Oct;27(10):1432-45