CGS 21680A
CGS 21680 HCL
CAS: 124431-80-7
Molecular Formula: C23H30ClN7O6
CGS 21680A - Names and Identifiers
CGS 21680A - Physico-chemical Properties
| Molecular Formula | C23H30ClN7O6 |
| Molar Mass | 535.9806 |
| Melting Point | 204-206°C |
| Solubility | DMSO (Slightly, Heated), Methanol (Slightly, Heated) |
| Appearance | Solid |
| Color | White to Light Beige |
| Storage Condition | Inert atmosphere,2-8°C |
| In vitro study | CGS 21680 HCl is an Adenosine A2 receptor agonist with an IC50 of 22 nM and a 140-fold higher selectivity than the A1 receptor. In the isolated rat heart perfusion model, CGS 21680 significantly increased coronary blood flow with an ED25 value of 1.8 nM.. CGS 21680 binds to the Adenosine A2 receptor with high affinity (Kd = 15.5 nM) and is saturated with binding to a single recognition site (apparent maximum binding = 375 fmol/mg protein). In hippocampal slices, CGS 21680 has a weaker agonist effect on presynaptic and postprocess electrophysiologic activity (a hypothetical Al receptor-mediated outcome), there was no effect in activating cAMP formation (assumed A2 mediated response). In striatal sections, CGS 21680 significantly activated cAMP formation with an EC50 of 110 nM, but had no effect on inhibition of electrical stimulation-induced dopamine release. CGS 21680A is in the form of the hydrochloride salt and CGS 21680C is the sodium salt of CGS 21680. CGS 21680 HCl is an Adenosine A2 receptor agonist with an IC50 of 22 nM and a 140-fold higher selectivity than the A1 receptor. In the isolated rat heart perfusion model, CGS 21680 significantly increased coronary blood flow with an ED25 value of 1.8 nM.. CGS 21680 binds to the Adenosine A2 receptor with high affinity (K d = 15.5 nM) and is saturated with binding to a single recognition site (apparent maximum binding = 375 fmol/mg protein). In hippocampal slices, CGS 21680 has a weaker agonist effect on presynaptic and postprocess electrophysiologic activity (a hypothetical Al receptor-mediated outcome), there was no effect in activating cAMP formation (assumed A2 mediated response). In striatal sections, CGS 21680 significantly activated cAMP formation with an EC50 of 110 nM, but had no effect on inhibition of electrical stimulation-induced dopamine release. CGS 21680A is in the form of the hydrochloride salt and CGS 21680C is the sodium salt of CGS 21680. |
| In vivo study | CGS 21680A was orally effective in spontaneously hypertensive rats at a dose of 10 mg/kg for up to 24 hours. CGS 21680A causes a transient (approximately 60 minutes) increase in heart rate in rats. CGS 21680 is a potent sedative for acetylcholine and glutamate receptors in rat cortical neurons. CGS 21680A was orally effective in spontaneously hypertensive rats at a dose of 10 mg/kg for up to 24 hours. CGS 21680A causes a transient (approximately 60 minutes) increase in heart rate in rats. CGS 21680 is a potent sedative for acetylcholine and glutamate receptors in rat cortical neurons. |
CGS 21680A - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.866 ml | 9.329 ml | 18.657 ml |
| 5 mM | 0.373 ml | 1.866 ml | 3.731 ml |
| 10 mM | 0.187 ml | 0.933 ml | 1.866 ml |
| 5 mM | 0.037 ml | 0.187 ml | 0.373 ml |
Last Update：2024-01-02 23:10:35
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