BIA 10-2474
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货号：A100075
BIA10-2474 is an inhibitor of fatty acid amide hydrolase (FAAH) with IC50 of 4.9 nM.
BIA 10-2474 化学结构
BIA 10-2474 3D分子结构
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BIA 10-2474 质控信息
URB-597
++++
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JNJ-1661010
+++
FAAH (rat), IC50: 10 nM
FAAH (human), IC50: 12 nM
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Biochanin A
+
FAAH (mouse), IC50: 1.8 μM
FAAH (human), IC50: 1.4 μM
EGFR
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PF-3845
++
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1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。
BIA 10-2474 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] 50 of 4.9 nM and shows IC50 values of 50-70 mg/kg (i.p.) in various rat brain regions[4] [5]
BIA 10-2474 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.
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BIA 10-2474 实验方案
计算器
摩尔计算器
总药量计算器
工作液计算器
存储液制备
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
BIA 10-2474 技术信息
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