同义名 :	-
	CAS号 :	1637300-25-4
	货号 :	A935740
	分子式 :	C21H20ClN5O
	纯度 :	98%+
	分子量 :	393.87
	MDL号 :	MFCD28411712
	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

GPR3 is orphan G-protein coupled receptor (GPCR) which results in elevated levels of cellular cAMP when overexpressing in heterologous expression systems as well as in primary neurons. AF64394 is a novel and selective GPR3 inverse agonist with pIC50 value of 7.3, 5.1 and 4.9 for GPR3, GPR6 and GPR12, respectively. AF34394 is specific and selective and thus forms useful tool for delineating the biology of GPR3. Whilst AF34394 is only of modest potency and relatively lipophilic (clogP = 5.2, LLE = 2.1), it shows promising SAR (structure activity relationship) and represents an excellent start point for further optimisation[1].

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	2.54mL 0.51mL 0.25mL	12.69mL 2.54mL 1.27mL	25.39mL 5.08mL 2.54mL

参考文献
[1]Jensen T, Elster L, Nielsen SM, Poda SB, Loechel F, Volbracht C, Klewe IV, David L, Watson SP. The identification of GPR3 inverse agonist AF64394; the first small molecule inhibitor of GPR3 receptor function. Bioorg Med Chem Lett. 2014 Nov 15;24(22):5195-8