| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
A2A receptor antagonist 1 is a novel and potent antagonist of the adenosine A2A receptor and A1 receptor with Kis of 4 and 264 nM, respectively. It is chemically related to the pyrazolo[3,4-d] and pyrrolo[2,3-d] pyrimidines. Highly selective against the human A(1) receptor subtype, A2A receptor antagonist 1 was found to be effective in an in vivo Parkinson's disease model.
| Targets |
adenosine A2A Receptor ( Ki = 4 nM ); A1 Receptor ( Ki = 264 nM )
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| ln Vitro |
A2A receptor antagonist 1 (CPI-444 analog) is a strong adenosine A2A receptor antagonist that exhibits binding activity with Ki values of 4 and 264 nM, respectively. It is selective over the A1 receptor[1].
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| ln Vivo |
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| References |
| Molecular Formula |
C16H12FN5O
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| Molecular Weight |
309.30
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| Exact Mass |
309.1
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| Elemental Analysis |
C, 62.13; H, 3.91; F, 6.14; N, 22.64; O, 5.17
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| CAS # |
443103-97-7
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| Related CAS # |
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| PubChem CID |
9879687
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| Appearance |
Solid powder
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| LogP |
2.3
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
23
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| Complexity |
414
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
JEEJMSUHUZNTCD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H12FN5O/c17-12-5-2-1-4-10(12)9-22-15-11(8-19-22)14(20-16(18)21-15)13-6-3-7-23-13/h1-8H,9H2,(H2,18,20,21)
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| Chemical Name |
1-[(2-fluorophenyl)methyl]-4-(furan-2-yl)pyrazolo[3,4-d]pyrimidin-6-amine
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| Synonyms |
A2A receptor antagonist 1; A2A-IN-1; A2A inhibitor 1
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| HS Tariff Code |
2934.99.03.00
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.08 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.08 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (8.08 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2331 mL | 16.1655 mL | 32.3311 mL | |
| 5 mM | 0.6466 mL | 3.2331 mL | 6.4662 mL | |
| 10 mM | 0.3233 mL | 1.6166 mL | 3.2331 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05501054 | Recruiting | Drug: Ipilimumab Drug: Nivolumab |
Renal Cell Carcinoma | M.D. Anderson Cancer Center | February 9, 2023 | Phase 1 Phase 2 |
| NCT05217498 | Not yet recruiting | Drug: Istradefylline Device: low oxygen therapy |
Spinal Cord Injuries Myelopathy |
Randy Trumbower, PT, PhD | September 1, 2024 | Phase 1 Phase 2 |
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