A2AR modulator-1
Based on 1 Customer Validation
A2AR modulator-1 (Compound 45) is a selective negative allosteric adenosine A2a receptor (A2aR) modulator with an IC50 value of 9 nM. A2AR modulator-1 reduces the affinity of endogenous adenosine for the receptor and inhibits cAMP signaling pathway activation. A2AR modulator-1 potently restores pCREB phosphorylation in CD4+ T cells, reversing immunosuppression in the tumor microenvironment, and shows potential to suppress tumor growth and metastasis in triple-negative breast cancer models.
For research use only. We do not sell to patients.
- Purity : 95.47%
- CAS No.: 3007566-23-3
- Formula: C23H20N6
- Molecular Weight:380.45
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
All Adenosine Receptor Isoforms
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Biological Activity
Description
IC50 & Target
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A2AR 9 nM (IC50) |
Chemical Information
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CAS No. 3007566-23-3
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Appearance Solid
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Molecular Weight 380.45
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Formula C23H20N6
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Color White to off-white
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SMILES
N#CC1=C(C2=CC=CC(C3=CC=CN=C3)=C2)C(C#N)=C(N4CCCCC4)N=C1N
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
In Vitro:
DMSO : 50 mg/mL (131.42 mM; Need ultrasonic; 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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)
In Vivo:
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.
In Vivo Dissolution Calculator
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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 (273 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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 (sealed storage, away from moisture). 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 | 2.6285 mL | 13.1423 mL | 26.2847 mL | 65.7117 mL |
| 5 mM | 0.5257 mL | 2.6285 mL | 5.2569 mL | 13.1423 mL | |
| 10 mM | 0.2628 mL | 1.3142 mL | 2.6285 mL | 6.5712 mL | |
| 15 mM | 0.1752 mL | 0.8762 mL | 1.7523 mL | 4.3808 mL | |
| 20 mM | 0.1314 mL | 0.6571 mL | 1.3142 mL | 3.2856 mL | |
| 25 mM | 0.1051 mL | 0.5257 mL | 1.0514 mL | 2.6285 mL | |
| 30 mM | 0.0876 mL | 0.4381 mL | 0.8762 mL | 2.1904 mL | |
| 40 mM | 0.0657 mL | 0.3286 mL | 0.6571 mL | 1.6428 mL | |
| 50 mM | 0.0526 mL | 0.2628 mL | 0.5257 mL | 1.3142 mL | |
| 60 mM | 0.0438 mL | 0.2190 mL | 0.4381 mL | 1.0952 mL | |
| 80 mM | 0.0329 mL | 0.1643 mL | 0.3286 mL | 0.8214 mL | |
| 100 mM | 0.0263 mL | 0.1314 mL | 0.2628 mL | 0.6571 mL |