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PF-2545920

Cat. No. M3447

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PF-2545920 Structure
Synonym:

Mardepodect; CAS# 898562-94-2

Size Price Availability Quantity
5mg USD 195  USD195 In stock
10mg USD 300  USD300 In stock
50mg USD 780  USD780 In stock
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Biological Activity

PF-2545920 a highly selective and potent PDE10A inhibitor with an IC50 of 0.37 nM. The PDE10A enzyme is expressed primarily in the brain, mostly in the striatum, nucleus accumbens and olfactory tubercle, and is thought to be particularly important in regulating the activity of dopamine-sensitive medium spiny neurons in the striatum which are known to be targets of conventional antipsychotic agents. n the conditioned avoidance response assay (CAR), PF-2545920 was active with an ED50 of 1 mg/kg. Administration of PF-2545920 to mice caused a dose dependent increase in striatal cGMP.

Protocol (for reference only)
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models Jugular vein-cannulated male Sprague-Dawley rats
Formulation 5:5:90 DMSO:1N HCl:saline
Dosages 0.1 mg/kg
Administration Inject intravenous through jugular vein catheter in a single dose 4 hours before feed
Chemical Information
Molecular Weight 392.45
Formula C25H20N4O
CAS Number 1292799-56-4
Solubility (25°C) DMSO 40 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Liliya Kopanitsa, et al. Suppression of Proliferation of Human Glioblastoma Cells by Combined Phosphodiesterase and Multidrug Resistance-Associated Protein 1 Inhibition

[2] Do-Yeon Kim, et al. The Potent PDE10A Inhibitor MP-10 (PF-2545920) Suppresses Microglial Activation in LPS-Induced Neuroinflammation and MPTP-Induced Parkinson's Disease Mouse Models

[3] Yanke Zhang, et al. The Phosphodiesterase 10A Inhibitor PF-2545920 Enhances Hippocampal Excitability and Seizure Activity Involving the Upregulation of GluA1 and NR2A in Post-synaptic Densities

[4] Jonathan M Wilson, et al. Phosphodiesterase 10A inhibitor, MP-10 (PF-2545920), produces greater induction of c-Fos in dopamine D2 neurons than in D1 neurons in the neostriatum

[5] Patrick R Verhoest, et al. Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia

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Keywords: PF-2545920, Mardepodect; CAS# 898562-94-2 supplier, PDE, inhibitors, activators

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