A cell-permeable pyrazoloquinoline compound that acts as a potent phosphodiesterase 10A inhibitor (Ki≤5nM against human PDE10A), while exhibiting >500-fold selectivity over other human PDEs 1-11 and little activity against CYP3A4 (IC50 >20uM) or a panel of 23 kinases (IC50 >30uM). Reported to be orally available in monkey and rat species and be efficacious in reversing nMDAR antagonist (+)-MK-801-induced hyperactivity in a ratsl (MED = 10mg/kg p.o.) in vivo.
Molecular Formula:C₁₈H₁₆ClN₅O
Solubility:DMSO
Molecular Weight:353.81
Primary Target Ki:≤5nM
Storage and Stability:May be stored at 4°C. For long-term storage, aliquot and store at 4°C. Do not freeze. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer.