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BIA 10-2474

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Chemical Structure| 1233855-46-3 同义名 : -
CAS号 : 1233855-46-3
货号 : A100075
分子式 : C16H20N4O2
纯度 : 99%+
分子量 : 300.356
MDL号 : MFCD30532661
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 2 mg/mL(6.66 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
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.