2. Metabolic Enzyme/Protease Apoptosis
  3. Prolyl Endopeptidase (PREP) Apoptosis
  4. 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.

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S 17092 Chemical Structure

S 17092 Chemical Structure

CAS No. : 176797-26-5

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Based on 1 publication(s) in Google Scholar

S 17092 Related Antibodies

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Description

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

S 17092 Related Antibodies

Cell Viability Assay[2]

Cell Line: N3-6-71, thymocytes and peripheral T cells of BALB/c mice
Concentration: 100 μM
Incubation Time: 2 h for thymocytes, 4 h for N3-6-71 and peripheral T cells
Result: Was able to entirely block activation-induced cell death (AICD) in N3-6-71 cells, inhibits the inducible activities of both caspase-8 and caspase-3.
Reduced PEP activity was observed as assessed by Suc-Gly-Pro-MCA cleavage in thymocytes.
Showed little or no toxicity when added alone at the concentrations tested in thymocytes.
Showed a reduced cell death in thymocytes and peripheral T cells.
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 (t1/2 > 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 3-5 months old male C57BL/6 mice[1]
Dosage: 10 mg/kg
Administration: Oral gavage (p.o.); twice daily for 7 days and 60 min prior to the training sessions
Result: Correct responses in the experimental group were 55, 58, and 74% in sessions 1, 2, and 3, respectively. Performance in experimental group was similar to that in non-amnesic controls.
Improved learning and memory performances in young amnesic C57BL/6 mice.
Animal Model: Adult male Macaca fascicularis monkeys treated with MPTP[1]
Dosage: 1, 3, 10 mg/kg
Administration: Oral gavage (p.o.); 7 days
Result: Significantly improved variable delayed response (VDR) performance (76.9% correct responses vs. post-MPTP only) at 3 mg/kg, but not at 1 or 10 mg/kg doses.
VDR performance tended to revert back to a normal delay-dependent pattern of response, performance significantly improved on shorter (2, 5, and 10 sec delay) but not on longer delay trials at the 3mg/kg dose. Improved performance on shorter delay trials was not seen with either the 1 or 10 mg/kg doses.
Significant improvements in DMS (delayed matching-to-sample) performance were observed after administration at either 3 or 10 mg/kg doses.
Significantly improved DA (delayed alternation) performance at the 3 mg/kg dose, from 79% at baseline to 90.6% after 7-days or longer treatments.
Animal Model: 21-22 and 25 months old C57BL/6 mice[1]
Dosage: 10 mg/kg
Administration: Oral gavage (p.o.); 7 days and again 1 h before each daily memory test
Result: With correct responses of 45 and 70% in control and experimental animals, respectively, in session 5 and 46 and 65%, respectively, in session 6 in 21-22 months old C57BL/6 mice.
Had a beneficial effect on the selective deficit observed 25 months old C57BL/6 mice.
Animal Model: Rats treated with scopolamine[1]
Dosage: 0.01-30 mg/kg
Administration: Intraperitoneal injection (i.p.); 60 or 120 min before session 1 then 24 h later 60 or 120 min before session 2, respectively
Result: Dose-dependently increased the retention time, alleviating scopolamine-induced amnesia. The maximum effect using 10 mg/kg with the 60 min pretest dosing interval was achieved using 3 mg/kg in the 120 min tests, suggesting that brain neuropeptide turnover may have been increased by increasing the time interval between the administration and the test.
Molecular Weight

384.53

Formula

C22H28N2O2S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C([C@H]1[C@@](C2=CC=CC=C2)([H])C1)N3[C@]4([H])[C@](CCCC4)([H])C[C@H]3C(N5CCSC5)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (260.06 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6006 mL 13.0029 mL 26.0058 mL
5 mM 0.5201 mL 2.6006 mL 5.2012 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6006 mL 13.0029 mL 26.0058 mL 65.0144 mL
5 mM 0.5201 mL 2.6006 mL 5.2012 mL 13.0029 mL
10 mM 0.2601 mL 1.3003 mL 2.6006 mL 6.5014 mL
15 mM 0.1734 mL 0.8669 mL 1.7337 mL 4.3343 mL
20 mM 0.1300 mL 0.6501 mL 1.3003 mL 3.2507 mL
25 mM 0.1040 mL 0.5201 mL 1.0402 mL 2.6006 mL
30 mM 0.0867 mL 0.4334 mL 0.8669 mL 2.1671 mL
40 mM 0.0650 mL 0.3251 mL 0.6501 mL 1.6254 mL
50 mM 0.0520 mL 0.2601 mL 0.5201 mL 1.3003 mL
60 mM 0.0433 mL 0.2167 mL 0.4334 mL 1.0836 mL
80 mM 0.0325 mL 0.1625 mL 0.3251 mL 0.8127 mL
100 mM 0.0260 mL 0.1300 mL 0.2601 mL 0.6501 mL
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S 17092 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

S 17092176797-26-5S 17092-1S17092S-17092Prolyl Endopeptidase (PREP)Apoptosisprolyl oligopeptidasePOPMemory enhancerProlyl endopeptidase inhibitorCognitive disordersNeuropeptidesNeuroprotectionCerebral agingInhibitorinhibitorinhibit

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