CB1/2 agonist 1
Based on 1 Customer Validation
CB1/2 agonist 1 is a potent and cross the blood-brain barrier CB1/2 agonist with EC50s of 56.15, 11.63 nM for CB1R and CB2R, respectively. CB1/2 agonist 1 reduces glutamate release and LPS-induced activation of microglial cells. CB1/2 agonist 1 shows anti-inflammatory and antinociceptive effects. CB1/2 agonist 1 has the potential for the research of multiple sclerosis.
For research use only. We do not sell to patients.
- Purity: 98.68%
- CAS No.: 2986688-90-6
- Formula: C21H24BrFN2O2
- Molecular Weight:435.33
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
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hCB1-R 56.15 nM (EC50) |
cannabinoid type-2 receptors 11.63 nM (EC50) |
CB1/2 agonist 1 (compound B2) (10 µM) inhibits AEA hydrolysis with an IC50 of 5.9 µM for FAAH[1].
CB1/2 agonist 1 shows high affinity for CB1R and CB2R with Kis of 2.9, 1.5 nM, respectively[1].
CB1/2 agonist 1 (10 µM) shows anti-inflammatory effect and significantly decreases the secretion of IL-1β and IL-6, increases the release of anti-inflammatory IL-10 to 483.7% in LPS-activated BV-2 cells[1].
CB1/2 agonist 1 (1, 10 µM) inhibits 4-AP-evoked glutamate release[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2986688-90-6
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Appearance Solid
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Molecular Weight 435.33
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Formula C21H24BrFN2O2
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Color White to off-white
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SMILES
CC1=C(C=C(C(N1CC2=CC=C(C=C2)F)=O)C(NC3CCCCCC3)=O)Br
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 20 mg/mL (45.94 mM; ultrasonic and warming and heat to 70°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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Purity & Documentation
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Data Sheet (272 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
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 | 2.2971 mL | 11.4855 mL | 22.9711 mL | 57.4277 mL |
| 5 mM | 0.4594 mL | 2.2971 mL | 4.5942 mL | 11.4855 mL | |
| 10 mM | 0.2297 mL | 1.1486 mL | 2.2971 mL | 5.7428 mL | |
| 15 mM | 0.1531 mL | 0.7657 mL | 1.5314 mL | 3.8285 mL | |
| 20 mM | 0.1149 mL | 0.5743 mL | 1.1486 mL | 2.8714 mL | |
| 25 mM | 0.0919 mL | 0.4594 mL | 0.9188 mL | 2.2971 mL | |
| 30 mM | 0.0766 mL | 0.3829 mL | 0.7657 mL | 1.9143 mL | |
| 40 mM | 0.0574 mL | 0.2871 mL | 0.5743 mL | 1.4357 mL |