S 17092

S 17092 (S 17092-1) is an orally active cerebral prolyl-endopeptidase (PEP) inhibitor with an IC₅₀ of 1.2 nM. S 17092 inhibits cell apoptosis. S 17092 mechanism of action is to inhibit the activity of PEP, slowing down the degradation of neuroactive peptides and thus enhancing memory function. S 17092 can be used for the research of memory impairment and cognitive disorders associated with cerebral aging^[1][2][3]. In Vitro:S 17092 produces inhibition of PEP activity in the cerebral cortex of Wistar rats; the minimal effective drug concentration is 0.1 nM^[1].
S 17092 (10^-7-10 μM) blocks the HEK 293 which displayed an intracellular PEP-like activity^[1].
S 17092 (100 μM, 2-4 h) prevents T cell receptor (TCR)-mediated apoptosis in cells, inhibits the inducible activities of both caspase-8 and caspase-3 in N3-6-71 cells^[2].
S-17092 (1-30 μM, 4 h) alone has no effect on ³H-CDPDAG accumulation, but it reverses the effect of lithium and carbachol with an EC₅₀ of 10 μM^[3].
In Vivo:S 17092 (1-10 mg/kg; p.o.; 7 days) improves the performance of cognitive tasks (VDR, DMS, DA) in a dose-dependent manner in MPTP (HY-15608)-treated monkeys^[1].
S 17092 (10 mg/kg; p.o.; 7 days and again 1 h before each daily memory test) alleviates the Scopolamine (HY-N0296)-induced memory deficit, improves learning and working memory performances in young, elderly and old C57BL/6 mice^[1].
S 17092 (0.01-30 mg/kg; i.p.; 60 or 120 min before session 1 then 24 h later 60 or 120 min before session 2, respectively) dose-dependently increases the retention time, alleviating scopolamine-induced amnesia in rats^[1].
S 17092 is a long acting PEP inhibitor (t_1/2 > 9 h). The 50% inhibitory dose (ID₅₀) for cortical PEP activity are 7.4 and 13.4 mg/kg at one hour after p.o. in Wistar rat and NMRI mouse, respectively^[1].