ADX-47273
Catalog No.S2690 Synonyms: BA 94673139
Molecular Weight(MW): 369.36
ADX47273 is a potent and specific mGlu5 positive allosteric modulator(PAM) with EC50 of 0.17 μM, showing no activity at other mGlu subtypes.
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Biological Activity
| Description | ADX47273 is a potent and specific mGlu5 positive allosteric modulator(PAM) with EC50 of 0.17 μM, showing no activity at other mGlu subtypes. | ||
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| In vitro |
ADX47273 causes a concentration-dependent increase in the response to 50 nM glutamate in HEK 293 cells expressing rat mGlu5, the maximal increase in the response is approximately 9-fold, with an EC50 of 0.17 ± 0.03 μM. ADX47273 causes a concentration-dependent increase in the response to 300 nM glutamate with an EC50 value of 0.23 ± 0.07 μM in primary astrocyte cultures. ADX47273 at concentration of 0.1 or 1 μM decreases the EC50 for glutamate for 4- and 9-fold, respectively, in HEK 293 cells expressing rat mGlu5. ADX47273 at concentration of 1 or 3 μM decreases the EC50 for glutamate for 4- and 9-fold, respectively, in primary astrocyte cultures. ADX47273 inhibits binding of [3H]MPEP to membranes prepared from HEK 293 cells expressing mGlu5 receptors with Ki of 4.3 ± 0.5 μM. [1] ADX-47273 at concentration of 0.3 μM elicited an enhancement of NMDA-receptor dependent long-term potentiation in rat hippocampal slices, the effect can be blocked in the presence of 10 μM specific mGlu5 receptor antagonist MPEP. [2] |
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| In vivo | ADX47273 intraperitoneally administrated at dose of 10 mg/kg increases ERK and CREB phosphorylation in both the prefrontal cortex and hippocampus in Long-Evans rats. ADX47273 intraperitoneally administrated at dose of 10-100 mg/kg produces dose-dependent decreases in avoidance responding and increased escapes at doses that did not produce any response failures in Sprague-Dawley rats. ADX47273 intraperitoneally administrated at dose of 10-300 mg/kg produces a dose-dependent decrease in apomorphine-induced climbing in CF-1 mice. ADX47273 intraperitoneally administrated at dose of 100 mg/kg decreased locomotor activity compared with vehicle pretreatment at 20 min after PCP, 30 min after apomorphine, and at all time points after amphetamine challenge in mice. ADX47273 intraperitoneally administrated at dose of 175 mg/kg lowers dopamine levels in the Sprague-Dawley rat nucleus accumbens. ADX47273 intraperitoneally administrated at dose of 1 to 50 mg/kg increases novel object recognition and reduces impulsivity in the five-choice serial reaction time test in rats. [1] ADX47273 intraperitoneally administrated at dose of 100 mg/kg significantly decreases conditioned avoidance response at 30 and 90 min post-injection in male Sprague-Dawley rats. [3] |
Protocol
| Animal Research: |
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Solubility (25°C)
| In vitro | DMSO | 74 mg/mL (200.34 mM) |
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| Ethanol | 30 mg/mL (81.22 mM) | |
| Water | Insoluble | |
| In vivo | Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 30% propylene glycol, 5% Tween 80, 65% D5W For best results, use promptly after mixing. |
30 mg/mL |
* 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.
Chemical Information
| Molecular Weight | 369.36 |
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| Formula | C20H17F2N3O2 |
| CAS No. | 851881-60-2 |
| Storage | powder |
| in solvent | |
| Synonyms | BA 94673139 |
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