A potent inhibitor of PDE10A
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Isomer(s)
42047PF-02545920
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PF-2545920

Item No. 18266

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[[4-[1-methyl-4-(4-pyridinyl)-1H-pyrazol-3-yl]phenoxy]methyl]-quinoline
CAS Number
898562-94-2
Molecular Formula
C25H20N4O
Formula Weight
392.5
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMF:PBS (pH 7.2) (1:20): 0.05 mg/mlDMSO: 15 mg/mlEthanol: 0.5 mg/ml
λmax
233, 317 nm
SMILES
CN1C=C(C2=CC=NC=C2)C(C(C=C3)=CC=C3OCC4=NC5=CC=CC=C5C=C4)=N1
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
InChi Key
AZEXWHKOMMASPA-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    10 mg

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    25 mg

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    Product Description

    PF-2545920 is a potent inhibitor of phosphodiesterase 10A (PDE10A; IC50 = 1.26 nM for the human recombinant enzyme).1 It is selective for PDE10A over other PDEs with IC50 values ranging from 1.7 to >10 μM. In vivo, PF-2545920 (0.1-3 mg/kg, i.p.) increases cAMP and cGMP production as well as phosphorylation of CREB and GluR1 in mouse striatum in a dose-dependent manner. It reduces climbing behavior induced by apomorphine (Item No. 16094) in mice (ID50 = 0.375 mg/kg) and disrupts the conditioned avoidance response in mice and rats (ID50s = 0.441 and 1.079 mg/kg, respectively). PF-2545920 reverses deficits in prepulse inhibition and social odor recognition induced by (+)-MK-801 (Item No. 10009019) in rats.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Grauer, S.M., Pulito, V.L., Navarra, R.L., et al. Phosphodiesterase 10A inhibitor activity in preclinical models of the positive, cognitive, and negative symptoms of schizophrenia. J. Pharmacol. Exp. Ther. 331(2), 574-590 (2009).