PDE10A Inhibitor, Cpd15

A cell-permeable pyrazoloquinoline compound that acts as a potent phosphodiesterase 10A inhibitor (K_i≤5 nM against human PDE10A-catalyzed cAMP hydrolysis), while exhibiting >500-fold selectivity over other human PDEs 1-11 and much reduced or little activity against CYP3A4 (IC₅₀ = 7.9 and >20 µM, respectively, with or without preincubation) as well as a panel of 23 kinases (IC₅₀ >30 µM). Reported to be orally available in monkey (AUC_{0-6 h} = 11,496 nM·h, T_1/2 = 7.1 h; 3 mg/kg p.o.) and rat (AUC_{0-6 h}475878) induced hyperactivity (1 h post p.o.) in a rat schizophrenia model (MED = 10 mg/kg p.o.) in vivo.

Cell permeable: yes

Reversible: yes

Packaged under inert gas

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

McElroy, W., et al. 2012. Bioorg. Med. Chem. Lett.22, 1335.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Toxicity: Standard Handling (A)