LY2183240
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
LY2183240是大麻素吸收高度有效的抑制剂(IC50值270 pM),也是脂肪酸酰胺水解酶(FAAH)的抑制剂(IC50值12.4 nM)[1]。
FAAH属于丝氨酸水解酶家族(是一个完整的膜酶)。酯酶和酰胺酶负责FAA家族信号脂(包括大麻素)的吸收。大麻素的吸收和代谢过程主要是通过FAAH获得的,因此FAAH的抑制可能导致大麻素吸收的障碍。
LY2183240是FAAH有效的共价抑制剂,具有阻碍大麻素吸收的效应。生化研究发现LY2183240通过FAAH的丝氨酸亲核试剂的氨甲酰化使FAAH失活[2]。在包含FAAH的细胞系中,放射物标记的3H-LY2183240对FAAH表现出有效的抑制性,抑制FAAH来阻碍大麻素的吸收。然而,在缺乏FAAH的HeLa细胞中,3H-LY2183240不结合FAAH,结果对大麻素吸收的阻碍非常弱。这表明LY2183240和FAAH的直接相互作用对于阻碍大麻素的吸收是必须的。然而,它也表明可能存在独立于FAAH的LY2183240调节大麻素吸收的无特征途径[1]。FAAH并不是LY2183240唯一的靶点,几个无特征的大脑丝氨酸水解酶也是LY2183240的靶点,这些可能是大麻素吸收的其他途径[2]。
在有疼痛的小鼠福尔马林试验中注射LY2183240(10 mg/kg)可以产生镇痛效应,这种疼痛与大脑大麻素水平升高有关。它表示LY2183240可能在体内抑制FAAH[2]。用LY2183240(10 mg/kg)处理小鼠90分钟,大脑组织的特征显示,LY2183240使FAAH和其他丝氨酸水解酶(分子大小为25 - 35 kDa)失活[2]。
参考文献:
[1] Dickason-Chesterfield A K et al., Pharmacological characterization of endocannabinoid transport and fatty acid amide hydrolase inhibitors. Cell Mol Neurobiol. 2006, 26(4-6): 407-23.
[2] Alexander J P, Cravatt B F. The putative endocannabinoid transport blocker LY2183240 is a potent inhibitor of FAAH and several other brain serine hydrolases. J Am Chem Soc. 2006, 128(30): 9699-9704.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 307.35 |
Cas No. | 874902-19-9 |
Formula | C17H17N5O |
Synonyms | LY 2183240; LY-2183240 |
Solubility | Soluble in DMSO |
Chemical Name | N,N-dimethyl-5-[(4-phenylphenyl)methyl]tetrazole-1-carboxamide |
SDF | Download SDF |
Canonical SMILES | CN(C)C(=O)N1C(=NN=N1)CC2=CC=C(C=C2)C3=CC=CC=C3 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
描述 | LY2183240是大麻素吸收高度有效的抑制剂,IC50值为270 pM。 | |||||
靶点 | anandamide uptake | fatty acid amide hydrolase (FAAH) | ||||
IC50 | 270 pM | 12.4 nM |