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    ADX-47273 (BA 94673139)
    ADX-47273 (BA 94673139)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1087
    CAS #: 851881-60-2Purity ≥98%

    Description: ADX47273 (ADX-47273; BA-94673139; BA94673139) is a potent, selective and specific mGlu5 positive allosteric modulator(PAM) with important biological activity. It activates mGlu5 with an EC50 of 0.17 μM, and exhibits no activity against other mGlu subtypes. In vivo, ADX47273 increased extracellular signal-regulated kinase and cAMP-responsive element-binding protein phosphorylation in hippocampus and prefrontal cortex, both of which are critical for glutamate-mediated signal transduction mechanisms.

    References: J Pharmacol Exp Ther. 2008 Dec;327(3):827-39; Pharmacol Biochem Behav. 2010 Mar;95(1):23-30. 

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    Molecular Weight (MW)369.36
    FormulaC20H17F2N3O2
    CAS No.851881-60-2
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 74 mg/mL (200.3 mM)
    Water:<1 mg/mL
    Ethanol: 30 mg/mL (81.2 mM)
    Solubility (In vivo)30% propylene glycol, 5% Tween 80, 65% D5W: 30 mg/mL
    SynonymsBA 94673139; ADX-47273; BA-94673139; BA94673139; ADX 47273; ADX47273


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    In Vitro

    In vitro activity: 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. 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.

    In VivoADX47273 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. 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. 
    Animal modelMale Long-Evans rats 
    Formulation & DosageDissolved in sterile 0.9% sodium chloride solution; 10 mg/kg; i.p. injection 
    References

    J Pharmacol Exp Ther. 2008 Dec;327(3):827-39; Pharmacol Biochem Behav. 2010 Mar;95(1):23-30. 


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    ADX-47273

    ADX47273 dose-dependently increased ERK and CREB phosphorylation in rat hippocampus and prefrontal cortex.


    ADX-47273

    ADX47273 was evaluated in the conditioned avoidance response in Sprague-Dawley rats. J Pharmacol Exp Ther. 2008 Dec;327(3):827-39. 
     

    ADX-47273

    ADX47273 evaluated in the apomorphine-induced climbing and stereotypy assay in CF-1 mice. J Pharmacol Exp Ther. 2008 Dec;327(3):827-39. 
     

    ADX-47273

    ADX47273 inhibits [3H]MPEP binding to rat mGlu5 receptor HEK cell membranes. J Pharmacol Exp Ther. 2008 Dec;327(3):827-39. 


    ADX-47273

    ADX47273 evaluated in the PCP-, apomorphine-, or amphetamine-induced locomotor activity in mice. J Pharmacol Exp Ther. 2008 Dec;327(3):827-39. 


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