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Technical Data
| Formula | C15H18N8O5 |
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| Molecular Weight | 390.35 | CAS No. | 313348-27-5 | |
| Solubility (25°C)* | In vitro | DMSO | 78 mg/mL (199.82 mM) | |
| Ethanol | 2 mg/mL (5.12 mM) | |||
| Water | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Biological Activity
| Description | Regadenoson (CVT-3146, Lexiscan) is a selective A2A adenosine receptor agonist with coronary vasodilating activity. | ||
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| Targets |
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| In vitro | Regadenoson has a relatively low binding affinity (hA2A Ki=290 nM) for human A2A receptors and greater than 30-fold selectivity versus the A2B and A3AR subtypes and 13-fold over the A1AR. Regadenoson behaves as a weak partial agonist causing cAMP accumulation in PC12 cells but as a full and potent agonist causing coronary vasodilation[1]. | ||
| In vivo | In a dog model, intravenous bolus injection of regadenoson causes a dose-dependent increase in myocardial blood flow and a dose-dependant decrease in coronary vascular resistance. In a rat heart model, regadenoson was shown to have a dose-dependent increase in heart rate and a decrease in mean arterial pressure at the higher doses. Regadenoson also caused more than a 2-fold increase in serum norepinephrine and epinephrine. For clinical data, Regadenoson has a volume of distribution of 11.5 L and 78.7 L (at steady-state), and an estimated clearance of 37.8 L/h. It is renally excreted (58% of total elimination) with a terminal half-life of 33 to 108 min[2]. |
Protocol (from reference)
References
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
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