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The A1, A2A, A2B, and A3 adenosine receptors (ARs) are ubiquitous G protein-coupled receptors. The four AR subtypes have been implicated in several areas of therapeutic interest such as stroke and other ischemic conditions, as well as inflammation, neurodegenerative diseases, diabetes, and sleep regulation. A3 AR antagonists are of interest as therapeutic agents in glaucoma agents and inflammation. CAY10498 is a potent and selective A3 AR antagonist exhibiting a Ki of 37 nM with 60 and 200-fold selectivity over A1 and A2A adenosine receptors, respectively. CAY10498 is also a structural analog of reversine, a dedifferentiation agent of embryonic progenitor cells. However, no dedifferentiation effects or any connection between A3 AR antagonism and dedifferentiation have been demonstrated.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 500 μg | $429 | 35 days | 35 days | |
| 1 mg | $790 | 35 days | 35 days | |
| 5 mg | $3,480 | 35 days | 35 days |
| Description | The A1, A2A, A2B, and A3 adenosine receptors (ARs) are ubiquitous G protein-coupled receptors. The four AR subtypes have been implicated in several areas of therapeutic interest such as stroke and other ischemic conditions, as well as inflammation, neurodegenerative diseases, diabetes, and sleep regulation. A3 AR antagonists are of interest as therapeutic agents in glaucoma agents and inflammation. CAY10498 is a potent and selective A3 AR antagonist exhibiting a Ki of 37 nM with 60 and 200-fold selectivity over A1 and A2A adenosine receptors, respectively. CAY10498 is also a structural analog of reversine, a dedifferentiation agent of embryonic progenitor cells. However, no dedifferentiation effects or any connection between A3 AR antagonism and dedifferentiation have been demonstrated. |
| Targets&IC50 | A3 (human):37 nM (Ki), A1AR (human):2.22 μM (Ki), A2A receptor (human):7.73 μM (Ki) |
| Molecular Weight | 320.39 |
| Formula | C18H20N6 |
| Cas No. | 863202-33-9 |
| Smiles | N(C1=C2C(=NC(NC3=CC=CC=C3)=N1)N=CN2)[C@H]4[C@@]5(C[C@](C4)(CC5)[H])[H] |
| Relative Density. | 1.403 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO: 10 mg/mL (31.21 mM), Sonication is recommended. DMSO:PBS (pH 7.2) (1:4): 0.2 mg/mL (0.62 mM), Sonication is recommended. DMF: 10 mg/mL (31.21 mM), Sonication is recommended. Ethanol: 1 mg/mL (3.12 mM), Sonication is recommended. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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