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BIA 10-2474 {[allProObj[0].p_purity_real_show]}

货号:A100075 Ambeed 开学季,买赠积分,赢豪礼

BIA10-2474 is an inhibitor of fatty acid amide hydrolase (FAAH) with IC50 of 4.9 nM.

BIA 10-2474 化学结构 CAS号:1233855-46-3
BIA 10-2474 化学结构
CAS号:1233855-46-3
BIA 10-2474 3D分子结构
CAS号:1233855-46-3
BIA 10-2474 化学结构 CAS号:1233855-46-3
BIA 10-2474 3D分子结构 CAS号:1233855-46-3
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BIA 10-2474 纯度/质量文件 产品仅供科研

货号:A100075 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 FAAH 其他靶点 纯度
URB-597 ++++

FAAH, IC50: 4.6 nM

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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 {[allProObj[0].p_purity_real_show]}
PF-3845 ++

FAAH, Ki: 230 nM

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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]. 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].

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.

BIA 10-2474 实验方案

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

CAS号1233855-46-3
分子式C16H20N4O2
分子量 300.356
别名
运输蓝冰
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

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