AM251

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Chemical Structure| 183232-66-8 同义名 : -
CAS号 : 183232-66-8
货号 : A800349
分子式 : C22H21Cl2IN4O
纯度 : 98%
分子量 : 555.24
MDL号 : MFCD01861181
存储条件：

Pure form Keep in dark place, sealed in dry, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(45.03 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
生物活性
靶点

  • CB1
描述 AM251 is a selective cannabinoid 1 (CB1) receptor antagonist with an IC50 of 8 nM. AM251 also acts as a potent GPR55 agonist with an EC50 of 39 nM[1].[2].[3].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03160326 - Recruiting March 2020 United States, California ... 展开 >> San Francisco VA Medical Center Recruiting San Francisco, California, United States, 94121 Contact: Julie Doyle    415-221-4810 ext 2597    Julie.Doyle2@va.gov    Principal Investigator: Cynthia Delgado, MD          United States, District of Columbia Washington DC VA Medical Center Recruiting Washington, District of Columbia, United States, 20422 Contact: Brian M Hoover, MS    202-745-8000 ext 55826    Brian.Hoover@va.gov    Principal Investigator: Michael Harris-Love, DSc          Sub-Investigator: Haniel Hernandez, DPT          Sub-Investigator: Sholey Argani, MD          Sub-Investigator: Marc Blackman, MD 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.80mL

0.36mL

0.18mL

9.01mL

1.80mL

0.90mL

18.01mL

3.60mL

1.80mL
参考文献

[1]Bruno A, et al. Beyond radio-displacement techniques for identification of CB1 ligands: the first application of afluorescence-quenching assay. Sci Rep. 2014 Jan 20;4:3757.

[2]Sharir H, et al. Pharmacological characterization of GPR55, a putative cannabinoid receptor. Pharmacol Ther. 2010 Jun;126(3):301-13.

[3]Thewke D, et al. AM-251 and SR144528 are acyl CoA:cholesterol acyltransferase inhibitors. Biochem Biophys Res Commun. 2009 Apr 3;381(2):181-6.

[4]Carey LM, et al. A pro-nociceptive phenotype unmasked in mice lacking fatty-acid amide hydrolase. Mol Pain. 2016 May 13;12. pii: 1744806916649192.

[5]Komaki A, et al. Study the Effect of Endocannabinoid System on Rat Behavior in Elevated Plus-Maze. Basic Clin Neurosci. 2015 Jul;6(3):147-53.