Balipodect (TAK063) is a highly effective and selective PDE10A inhibitor (IC50: 0.30 nM); Its selectivity is >15000-fold over other PDEs.

PDE10A:0.3 nM

TAK-063在小鼠中具有高脑穿透能力。通过口服TAK-063给小鼠，在0.3 mg/kg的剂量下，TAK-063能显著提高纹状体中的cAMP和(cGMP)水平，并在最小有效剂量(MED)0.3 mg/kg时，有效抑制由苯环利定(phencyclidine, PCP)引起的高运动性。目前，TAK-063治疗精神分裂症[正处于临床实验阶段[1]。

Catalytic assay: MEK5 protein isolated from a baculovirus expression system is used to measure kinase activity utilizing PKLight ATP Detection Reagent. The assay is performed using 15 nM GST-MEK5 and 0.75 μM ATP in assay buffer consisting of 25 mM Hepes, pH 7.5, 10 mM MgCl2, 50 mM KCl, 0.2% BSA, 0.01% CHAPS, 100 μM Na3VO4, 0.5 mM DTT and 1% DMSO in the presence of varying concentrations of BIX02188. The kinase reaction mixture is incubated for 90 minutes at room temperature followed by addition of 10 μL of an ATP detection reagent for 15 minutes. The relative light unit (RLU) signal is measured and the RLU signals are converted to percent of control (POC) values for the determination of IC50 value.