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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。 |
靶点 |
|
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]. |
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 << |
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 |
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 |