LY2183240
(Synonyms: 5-([1,1'-联苯]-4-甲基)-N,N-二甲基-1H-四氮唑-1-甲酰胺,LY 2183240; LY-2183240) 目录号 : GC15094A potent, competitive inhibitor of anandamide uptake
Cas No.:874902-19-9
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
LY2183240 is a highly potent blocker of anandamide uptake with IC50 value of 270 pM, and an inhibitor of fatty acid amide hydrolase (FAAH) activity with IC50 value of 12.4 nM [1].
Fatty acid amide hydrolase (FAAH) belongs to the family of serine hydrolase, which is an integral membrane enzyme. It has esterase and amidase activity that are responsive for the uptake of fatty acid amide (FAA) family signaling lipids, including anandamide. The uptake and metabolic process of anandamide is mainly achieved by FAAH, therefore the inhibition of FAAH may result in the blockage of anadaminde uptake.
LY2183240 is a potent and covalent inhibitor of FAAH, with the effect of blocking anandamide uptake. Biochemical research had identified that LY2183240 inactivate FAAH via carbamylation of the serine nucleophile of FAAH [2]. In RBL cell line containing FAAH, radioactive labeled 3H-LY2183240 exhibited strong binding to FAAH, inhibition of FAAH and thus blockage of anandamide uptake. However, in HeLa cells lacking FAAH, 3H-LY2183240 was less bound, and the blockage of anandamide uptake was very weak. It suggested that the direct interaction between LY2183240 and FAAH was required to block the anandamide uptake. However, it also indicated that there might be uncharacterized pathways of anandamide uptake regulated by LY2183240, independent from FAAH [1]. However, FAAH is not the sole target for LY2183240. Several uncharacterized brain serine hydrolases were also identified as the target of LY2183240, and these might be additional pathway for anandamide uptake [2].
In mouse model, 10 mg/kg injection of LY2183240 would produce analgesic effects in the formalin test of noxious pain which is a phenotype associated with elevated level of anandamide in brain. It indicated LY2183240 might inhibit FAAH in vivo [2]. When mice were administrated with LY2183240 (10 mg/kg, ip) for 90 min, characterization of brain tissues revealed that LY2183240 inactivated FAAH and other brain serine hydrolases ranging from 25-35 kDa [2].
References:
[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.
Cas No. | 874902-19-9 | SDF | |
别名 | 5-([1,1'-联苯]-4-甲基)-N,N-二甲基-1H-四氮唑-1-甲酰胺,LY 2183240; LY-2183240 | ||
化学名 | N,N-dimethyl-5-[(4-phenylphenyl)methyl]tetrazole-1-carboxamide | ||
Canonical SMILES | CN(C)C(=O)N1C(=NN=N1)CC2=CC=C(C=C2)C3=CC=CC=C3 | ||
分子式 | C17H17N5O | 分子量 | 307.35 |
溶解度 | DMF: 3 mg/ml,DMSO: 2 mg/ml,Ethanol: 10 mg/ml,Ethanol:PBS(pH 7.2) (1:5): 0.1 mg/ml | 储存条件 | Store at -20°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
||
Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 3.2536 mL | 16.2681 mL | 32.5362 mL |
5 mM | 0.6507 mL | 3.2536 mL | 6.5072 mL |
10 mM | 0.3254 mL | 1.6268 mL | 3.2536 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。