AM281
Based on 1 publication(s) in Google Scholar
AM281 is a selective CB1 receptor antagonist with an IC50 of 9.91 nM. AM281 inhibits CB2 receptor with an IC50 of 13000 nM.
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- 純度: 98.60%
- CAS 番号: 202463-68-1
- 分子式: C21H19Cl2IN4O2
- 分子量:557.21
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 AM281
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生物活性
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CB1 9.91 nM (IC50) |
CB2 13000 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
13.6 μM
Compound: 6, AM281
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Agonist activity at human GPR55 expressed in HEK293 cells assessed as increase in oscillation Ca2+ transients by fura-2 dye based fluorescence analysis
Agonist activity at human GPR55 expressed in HEK293 cells assessed as increase in oscillation Ca2+ transients by fura-2 dye based fluorescence analysis
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10.1039/C3MD00394A |
AM281 (0.01-10 μM) promotes a concentration dependent increase in 10 μM Aβ 25-35 induced neurotoxicity in SH-SY5Y cells in the presence of 10 μM KSO 1-6[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chronic administration of AM281 at 2.5 mg/kg improves recognition index to the 22.1±4.8 and single dose of AM281 at 5 mg/kg improves the memory impairment to the 8.5±4, as compared with vehicle-treated which is 4.8±2.5. Administration of AM281 at a dose of 2.5 mg/kg in chronic form and 5 mg/kg in acute dose improve memory[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male NMRI mice with the weight of 25-30 g[3]
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Dosage:0.62, 1.25 and 2.5 mg/kg (chronic administration); 2.5, 5 and 10 mg/kg (acute administration)
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Administration:Administrated i.p. every day concurrently with morphine except the day of experiment (chronic administration); Singly injected 40 min before second trial (acute administration)
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Result:The simultaneous daily administration of AM281 with morphine significantly shortened the exploration time, as compared with morphine-dependent mice receiving vehicle.
Acute administration at a dose of 5 mg/kg, significantly augmented recognition index.
化学情報
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CAS 番号 202463-68-1
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性状 Solid
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分子量 557.21
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分子式 C21H19Cl2IN4O2
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Color White to light yellow
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SMILES
O=C(C1=NN(C2=CC=C(Cl)C=C2Cl)C(C3=CC=C(I)C=C3)=C1C)NN4CCOCC4
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Mol Pain
EXPRESS: CB2 receptor agonist AM1241 regulating the polarization of microglia reduces morphine tolerance through IL-4/STAT6 pathway. [Abstract]2025 Aug 18:17448069251374281. PMID: 40823889
溶剤 & 溶解度
DMSO : 7.14 mg/mL (12.81 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (278 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. K S S Dossou, et al. Development and preliminary validation of a plate-based CB1/CB2 receptor functional assay. Anal Biochem. 2013 Jun 15;437(2):138-43. [Content Brief]
[3]. G Vaseghi, et al. The effect of AM281, a cannabinoid antagonist, on memory performance during spontaneous morphine withdrawal in mice. Res Pharm Sci. 2013 Jan;8(1):59-64. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7947 mL | 8.9733 mL | 17.9466 mL | 44.8664 mL |
| 5 mM | 0.3589 mL | 1.7947 mL | 3.5893 mL | 8.9733 mL | |
| 10 mM | 0.1795 mL | 0.8973 mL | 1.7947 mL | 4.4866 mL |
AM281 関連分類
HY-13505 関連分類
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