A2AR-antagonist-1
Based on 1 Customer Validation
A2AR-antagonist-1 (compound 38) is an orally active adenosine A2A receptor (A2AR) antagonist (IC50=29 nM). A2AR-antagonist-1 exhibits anti-tumor activity and mouse liver microsomal metabolic stability (t1/2=86.1 min). A2AR-antagonist-1 is also a T cells activator, via inhibiting immunosuppressive molecules (LAG-3 and TIM-3) and enhancing effector molecules (GZMB, IFNG, and IL-2).
For research use only. We do not sell to patients.
- Purity: 96.68%
- CAS No.: 2922920-71-4
- Formula: C27H25N5O2
- Molecular Weight:451.52
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Storage:Powder -20°C, 3 years , 4°C, 2 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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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A2AR 29 nM (IC50) |
A2AR-antagonist-1 (0.001-10 μM; 30 min) decreases the level of phosphorylated ERK induced by NECA in HEK293-A2AR cells[1].
A2AR-antagonist-1 (0.1-10 μM; 5 h) inhibits NECA-induced immunological molecules expression and increases effector molecules expression in Jurkat T cells (human immortalized T lymphocyte cell line)[1].
A2AR-antagonist-1 (0.1-10 μM; 48 h) recovers impairment of cytotoxic function of OT-I mouse splenocyte (OT-I CTL) against MC38-OVA cells, enhances T cell’s activation and effector function in vitro[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Jurkat T cells
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Concentration:0.1 μM, 1 μM, and 10 μM
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Incubation Time:5 hours
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Result:Reversed NECA (1 μM)-induced up-regulation of immunosuppressive molecules (LAG-3 and TIM-3), and NECA-induced down-regulation of effector molecules (GZMB, IFNG, and IL-2).
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Cell Line:Cytotoxic T lymphocytes from OT-I mouse splenocyte (OT-I CTL)
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Concentration:0.1 μM, 1 μM, and 10 μM
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Incubation Time:48 hours
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Result:Increased relative killing ability of OT-I CTL according to image.
Pharmacokinetic Analysis in mouse[1]
| Route | Dose (mg/kg) | Cmax (ng/mL) | AUC0-last (ng·h/mL) | AUC0-t (ng·h/mL) | t1/2 (h) | F (%) |
| i.v. | 2 | 2584 | 5577 | 5565 | 0.93 | / |
| p.o. | 10 | 8823 | 24008 | 24003 | 2.35 | 86.1 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MC38 xenograft model in mouse[1]
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Dosage:100 mg/kg
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Administration:PO; once daily for 23 days
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Result:Promoted CD8+ T cell accumulation.
Enhanced antitumor immunity, promoted tumor regression.
Had insignificant effect on body weight of the mice.
Chemical Information
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CAS No. 2922920-71-4
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Appearance Solid
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Molecular Weight 451.52
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Formula C27H25N5O2
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Color White to off-white
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SMILES
O=C(N(CC1=CC=CC(C(O)(C)C)=C1)C=C2)C=C2C3=NC(N)=NC(C4=C(C)C(C#N)=CC=C4)=C3
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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 : 25 mg/mL (55.37 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. 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)
Purity & Documentation
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Data Sheet (275 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. 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 | 2.2147 mL | 11.0737 mL | 22.1474 mL | 55.3685 mL |
| 5 mM | 0.4429 mL | 2.2147 mL | 4.4295 mL | 11.0737 mL | |
| 10 mM | 0.2215 mL | 1.1074 mL | 2.2147 mL | 5.5369 mL | |
| 15 mM | 0.1476 mL | 0.7382 mL | 1.4765 mL | 3.6912 mL | |
| 20 mM | 0.1107 mL | 0.5537 mL | 1.1074 mL | 2.7684 mL | |
| 25 mM | 0.0886 mL | 0.4429 mL | 0.8859 mL | 2.2147 mL | |
| 30 mM | 0.0738 mL | 0.3691 mL | 0.7382 mL | 1.8456 mL | |
| 40 mM | 0.0554 mL | 0.2768 mL | 0.5537 mL | 1.3842 mL | |
| 50 mM | 0.0443 mL | 0.2215 mL | 0.4429 mL | 1.1074 mL |
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