FIGURE 6.
Thiamet G vs. MK-8719 and L01. OGA inhibitors (thiamet G and MK-8719) and OGT inhibitor L01 are compared here. Both thiamet G and MK-8917 have low Ki and EC50, and both are highly selective for OGA; MK has a higher cellular permeability and brain-to-plasma ratio, although it is not yet commercially available, and thus, fewer studies have used MK-8917. OGT inhibitors are still with Ki/IC50 of µM range and not commercially available, and no in vivo studies have been reported yet.