CTP499, a selective PDE inhibitor, and the deuterium-containing agent is an HDX analogue and a metabolite of hexantheobromine that slows the progression of type 2 diabetic nephropathy in patients with macroalbuminuria.
JTP-4819 is a potent and selective prolyl endopeptidase (PEP) inhibitor with potential for treating Alzheimer's disease. At nanomolar concentration, JTP-4819 inhibited the degradation of substance P, arginine-vasopressin, and thyrotropin-releasing hormone by PEP in supernatants of the rat cerebral cortex and hippocampus. Repeated administration of JTP-4819 reversed the aging-induced decrease in brain substance P-like and thyrotropin-releasing hormone-like immunoreactivity, suggesting that this drug may be able to improve the imbalance of peptidergic neuronal systems that develops with senescense by inhibiting PEP activity. JTP-4819 increased acetylcholine release from the frontal cortex and hippocampus, regions closely associated with memory, in both young and aged rats.
ETP 45835 dihydrochloride is a Mnk2 and Mnk1 inhibitor (IC50 values are 575 and 646 nM respectively). Exhibits selectivity against a panel of 24 protein Ki nases, including those upstream of Mnk1 2.