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PF-2545920

Cat. No. M3447

PF-2545920 Structure
Size Price Availability Quantity
5mg USD 220 In stock
10mg USD 300 In stock
50mg USD 780 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
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
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 392.45
Formula C25H20N4O
CAS Number 1292799-56-4
Purity >99%
Solubility DMSO 70 mg/mL
Storage at -20°C
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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: PF-2545920 supplier, PDE, inhibitors

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