Mardepodect (hydrochloride)

PF-2545920 (hydrochloride)

C25H21ClN4O

DMSO : 25 mg/mL (58.29 mM; Need ultrasonic)

Metabolic Enzyme/Protease

Mardepodect hydrochloride (PF-2545920 hydrochloride) is a potent and selective PDE10A inhibitor with an IC₅₀ of 0.37 nM, with >1000-fold selectivity over the PDE. IC50 & Target: IC50: 0.37 nM (PDE10A)^[1]. In Vivo: 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), Mardepodect (PF-2545920) was active with an ED50 of 1 mg/kg. Administration of Mardepodect (PF-2545920) to mice caused a dose dependent increase in striatal cGMP.