Catalog No.: PC-49494Not For Human Use, Lab Use Only.
MK-8189 (Elpipodect, MK8189) is a highly potent, selective PDE10A inhibitor with Ki of 29 pM, 500,000-fold selectivity over the other PDE enzyme families (PDE1-PDE11).
MK-8189 (Elpipodect, MK8189) is a highly potent, selective PDE10A inhibitor with Ki of 29 pM, 500,000-fold selectivity over the other PDE enzyme families (PDE1-PDE11).
MK-8189 shows an IC50 of 1.6 nM in cells recombinantly expressing full-length human PDE10A.
MK-8189 has an excellent profile against ion channels (Iks, Cav1.2, and Nav1.5 >30 μM, and functional hERG Ikr IC50=33 μM). One off-target activity was identified in a broad Panlabs panel (somatostatin receptor type 2 (SSTR2) IC50=2.8 μM in a radioligand binding assay).
MK-8189 (0.25 mg/kg, oral) attenuates MK-801-induced locomotor activity in rats.
