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AM251 {[allProObj[0].p_purity_real_show]}

货号:A800349

AM251 是一种选择性的大麻素 1 (CB1) 受体拮抗剂,IC50 为 8 nM,并且也是一种有效的 GPR55 激动剂,EC50 为 39 nM。

AM251 化学结构 CAS号:183232-66-8
AM251 化学结构
CAS号:183232-66-8
AM251 3D分子结构
CAS号:183232-66-8
AM251 化学结构 CAS号:183232-66-8
AM251 3D分子结构 CAS号:183232-66-8
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AM251 纯度/质量文件 产品仅供科研

货号:A800349 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 CB1 CB2 其他靶点 纯度
Otenabant HCl ++++

rCB1, Ki: 2.8 nM

hCB1, Ki: 0.7 nM

98+%
AM251 98%
Rimonabant +++

hCB1, IC50: 13.6 nM

++

hCB2, IC50: 1.64 μM

98%
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。

AM251 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].
体内研究

AM251, at a dosage of 3 mg/kg administered intraperitoneally, significantly decreases capsaicin-evoked nocifensive behavior in a genotype-dependent manner. AM251 (3 mg/kg, i.p.) reduces the duration of heat hypersensitivity in FAAH KO but not WT mice. AM251 suppresses capsaicin-evoked heat hypersensitivity in a time-dependent manner in FAAH KO but not in WT mice. Post-hoc analysis reveals that FAAH KO mice receiving vehicle (i.p.) display heightened thermal hypersensitivity at 30, 60, and 90 minutes post-capsaicin in comparison to FAAH KO animals receiving AM251)[4].

Furthermore, AM251 influences anxiety-related behaviors in rats, as indicated by its impact on open arm entries and time spent in the open arms of an elevated plus maze. Significant reductions in these measures were noted at doses of 1 mg/kg and 5 mg/kg, suggesting anxiogenic effects at these concentrations[5].

体外研究

AM251 shows an agonist response in HEK293 cells, similar to that found in the yeast expression system[2].

In macrophages, both unstimulated and stimulated by acetylated LDL, AM251 reduces cholesteryl ester synthesis. This effect is observed regardless of the presence or absence of CB2 receptors, indicating a broader scope of action beyond just cannabinoid receptor interaction[3].

AM251 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 <<

AM251 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.

AM251 实验方案

计算器
存储液制备 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

AM251 技术信息

CAS号183232-66-8
分子式C22H21Cl2IN4O
分子量 555.239
别名
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

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

动物实验配方
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