同义名 :	-
	CAS号 :	1233855-46-3
	货号 :	A100075
	分子式 :	C16H20N4O2
	纯度 :	99%+
	分子量 :	300.36
	MDL号 :	MFCD30532661
	存储条件：	Pure form Inert atmosphere, 2-8°C In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-

生物活性

描述

Fatty acid amide hydrolase (FAAH), an integral membrane bound enzyme and a member of the extensive family of serine hydrolases referred to as amidase signature (AS) family, catalyses degradation of lipid signalling fatty acid amides including the sleep-inducing oleamide and endogenous cannabinoid anandamide (AEA)[3]. BIA10-2474 is an inhibitor of fatty acid amide hydrolase (FAAH) with IC50 of 4.9 nM and shows IC50 values of 50-70 mg/kg (i.p.) in various rat brain regions[4]. BIA 10-2474 (50 mM) changed FAAH substrates (N-acylethanolamines), as well as several other lipid classes, including triglycerides, monoacylglycerols, (lyso) phosphatidylcholines, free fatty acids, and plasmalogens in human cortical neuron, which suggests BIA 10-2474 has the potential to cause metabolic dysregulation in the nervous system[5].

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	3.33mL 0.67mL 0.33mL	16.65mL 3.33mL 1.66mL	33.29mL 6.66mL 3.33mL

参考文献

[1]van Esbroeck ACM, Janssen APA, et al. Activity-based protein profiling reveals off-target proteins of the FAAH inhibitor BIA 10-2474. Science. 2017 Jun 9;356(6342):1084-1087. [2]Kerbrat A, Ferre JC, et al. Acute Neurologic Disorder from an Inhibitor of Fatty Acid Amide Hydrolase. N Engl J Med. 2016 Nov 3;375(18):1717-1725. [3]McKinney MK, Cravatt BF. Structure and function of fatty acid amide hydrolase. Annu Rev Biochem. 2005;74:411-32. doi: 10.1146/annurev.biochem.74.082803.133450. PMID: 15952893. [4]Tong J, Mizrahi R, Houle S, Kish SJ, Boileau I, Nobrega J, Rusjan PM, Wilson AA. Inhibition of fatty acid amide hydrolase by BIA 10-2474 in rat brain. J Cereb Blood Flow Metab. 2017 Nov;37(11):3635-3639. doi: 10.1177/0271678X16668890. Epub 2016 Oct 1. PMID: 27650910; PMCID: PMC5669339. [5]van Esbroeck ACM, Janssen APA, Cognetta AB 3rd, Ogasawara D, Shpak G, van der Kroeg M, Kantae V, Baggelaar MP, de Vrij FMS, Deng H, Allarà M, Fezza F, Lin Z, van der Wel T, Soethoudt M, Mock ED, den Dulk H, Baak IL, Florea BI, Hendriks G, De Petrocellis L, Overkleeft HS, Hankemeier T, De Zeeuw CI, Di Marzo V, Maccarrone M, Cravatt BF, Kushner SA, van der Stelt M. Activity-based protein profiling reveals off-target proteins of the FAAH inhibitor BIA 10-2474. Science. 2017 Jun 9;356(6342):1084-1087. doi: 10.1126/science.aaf7497. PMID: 28596366; PMCID: PMC5641481.