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    Mardepodect (PF-2545920; MP-10)
    Mardepodect (PF-2545920; MP-10)

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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 #: V0792
    CAS #: 898562-94-2Purity ≥98%

    Description: Mardepodect (formerly known as PF-2545920, PF2545920, MP10; MP-10) is a novel, potent and selective PDE10A (phosphodiesterase) inhibitor with antipsychotic activity. It inhibits PDE10A with an IC50 of 0.37 nM, and shows >1000-fold selectivity for PDE10A over other isoforms of PDE. It is potentially useful for the treatment of schizophrenia. 

    References: J Pharmacol Exp Ther. 2009 Nov;331(2):574-90; J Med Chem. 2009 Aug 27;52(16):5188-96.

    Related CAS: 1292799-56-4

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    Molecular Weight (MW)392.45
    FormulaC25H20N4O
    CAS No.898562-94-2
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 78 mg/mL (198.8 mM)
    Water:<1 mg/mL
    Ethanol: 78 mg/mL (198.8 mM)
    SMILESCN1N=C(C2=CC=C(OCC3=NC4=CC=CC=C4C=C3)C=C2)C(C5=CC=NC=C5)=C1
    SynonymsMardepodect; PF-2545920; PF 2545920; MP-10; MP10; MP 10; PF2545920; 

    Chemical Name: 2-(4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)phenoxymethyl)quinoline

    InChi Key: AZEXWHKOMMASPA-UHFFFAOYSA-N

    InChi Code: InChI=1S/C25H20N4O/c1-29-16-23(18-12-14-26-15-13-18)25(28-29)20-7-10-22(11-8-20)30-17-21-9-6-19-4-2-3-5-24(19)27-21/h2-16H,17H2,1H3

    SMILES Code: CN1N=C(C2=CC=C(OCC3=NC4=CC=CC=C4C=C3)C=C2)C(C5=CC=NC=C5)=C1           


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    In Vitro

    In vitro activity: PF-2545920 (Also known as Mardepodect, MP-10) is a potent and selective PDE10A (phosphodiesterase) inhibitor with IC50 of 0.37 nM, and with >1000-fold selectivity over the PDE. It is potentially useful for the treatment of schizophrenia. PF-2545920 is active in a range of antipsychotic models, antagonizing apomorphine-induced climbing in mice, inhibiting conditioned avoidance responding in both rats and mice, and blocking N-methyl-D-aspartate antagonist-induced deficits in prepulse inhibition of acoustic startle response in rats, while improving baseline sensory gating in mice. PF-2545920 intraperitoneally administrated at dose of 0.3, 3, and 5 mg/kg in male CF-1 mice causes striking increases in GluR1 phosphorylation levels of 3-, 5.4-, and 4.1-fold , respectively. MP-10 at concentration of 1 μM treats Rat striatal slices for 30 min, the level of GluR1S845 phosphorylation at the cell surface is significantly increased 2-fold, without change the level of total GluR1 on the cell surface. MP-10 intraperitoneally administrated at dose of 0.3, 3, and 5 mg/kg in male CF-1 mice results in robust, statistically significant increases in CREBS133 phosphorylation of 3-, 4-, and 2.6-fold, respectively. MP-10 intraperitoneally administrated at dose of 3 mg/kg increases both enkephalin and substance-P mRNA levels in striatum of CF-1 mice. MP-10 intraperitoneally administrated at dose of 0.3-1 mg/kg decreases avoidance responding with a significant treatment effect in the mouse CAR model. Mice treated with MP-10 at dose of 0.03 mg/kg spents more time in the empty than social side in the mice, MP-10 also dose-dependently decreased locomotor activity.


    Kinase Assay: PF-2545920 (Also known as Mardepodect, MP-10) is a potent and selective PDE10A (phosphodiesterase) inhibitor with IC50 of 0.37 nM, and with >1000-fold selectivity over the PDE.

    In VivoPF-2545920 is shown to be efficacious both in vitro and in vivo with improved penetration in CNS. It has excellent in vivo efficacy in neurochemical elevation of cyclic nucleotides and in models predictive of antipsychotic activity. Administration of PF-2545920 to mice can cause increase in striatal cGMP with the minimal effective dose at about 1mg/kg.
    Animal modelJugular vein-cannulated male Sprague-Dawley rats
    Formulation & Dosage Dissolved in 5:5:90 DMSO:1N HCl:saline; 0.1 mg/kg; i.v. injection
    ReferencesJ Pharmacol Exp Ther. 2009 Nov;331(2):574-90; J Med Chem. 2009 Aug 27;52(16):5188-96.


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

    PF-2545920

    Dose-dependent effects of PDE10 inhibitors upon mouse striatal cyclic nucleotide levels. J Pharmacol Exp Ther.2009 Nov;331(2):574-90.

    PF-2545920

    Dose-dependent effects of PDE10 inhibitors upon mouse striatal CREBS133 and DARPP-32T34 phosphorylation. J Pharmacol Exp Ther. 2009 Nov;331(2):574-90.
     


    PF-2545920

    Acute treatment with MP-10 increases GluR1S845 phosphorylation levels at the cell surface in rat striatal slices. J Pharmacol Exp Ther. 2009 Nov;331(2):574-90.

    PF-2545920


    MP-10 activates both the D1-direct and D2-indirect pathway. J Pharmacol Exp Ther.2009 Nov;331(2):574-90.

    PF-2545920


    Papaverine and MP-10 disrupt CAR in rats and mice. J Pharmacol Exp Ther. 2009 Nov;331(2):574-90.

    PF-2545920


    Papaverine and MP-10 increase time spent in the social chamber in SASA. J Pharmacol Exp Ther. 2009 Nov;331(2):574-90.


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