S 17092
Based on 1 publication(s) in Google Scholar
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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.78%
- CAS. Nr.: 176797-26-5
- Formel: C22H28N2O2S
- Molecular Weight:384.53
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) S 17092
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Biologische Aktivität
Beschreibung
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. Further protocols information, click here.
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Cell Line:N3-6-71, thymocytes and peripheral T cells of BALB/c mice
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Concentration:100 μM
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Incubation Time:2 h for thymocytes, 4 h for N3-6-71 and peripheral T cells
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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 (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.
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Animal Model:3-5 months old male C57BL/6 mice[1]
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Dosage:10 mg/kg
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Administration:Oral gavage (p.o.); twice daily for 7 days and 60 min prior to the training sessions
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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.
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Animal Model:Adult male Macaca fascicularis monkeys treated with MPTP[1]
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Dosage:1, 3, 10 mg/kg
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Administration:Oral gavage (p.o.); 7 days
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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.
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Animal Model:21-22 and 25 months old C57BL/6 mice[1]
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Dosage:10 mg/kg
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Administration:Oral gavage (p.o.); 7 days and again 1 h before each daily memory test
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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.
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Animal Model:Rats treated with scopolamine[1]
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Dosage:0.01-30 mg/kg
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Administration:Intraperitoneal injection (i.p.); 60 or 120 min before session 1 then 24 h later 60 or 120 min before session 2, respectively
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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.
Chemical Information
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CAS. Nr. 176797-26-5
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Appearance Solid
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Molecular Weight 384.53
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Formel C22H28N2O2S
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Color White to off-white
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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
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Synonyms
S 17092-1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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J Med Chem
Structure-Guided Optimization of 4-Chloro-Pyrazolopyridine Analogs for Covalent PREP Inhibition. [Abstract]2026 Jan 22;69(2):1303-1321. PMID: 41512187
Lösungsmittel & Löslichkeit
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.
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.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Protokoll
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
Reinheit & Dokumentation
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Data Sheet (286 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Philippe Morain, et al. S 17092: a prolyl endopeptidase inhibitor as a potential therapeutic drug for memory impairment. Preclinical and clinical studies. CNS Drug Rev. Spring 2002;8(1):31-52. [Content Brief]
[2]. Odaka C, et al. Murine T cells expressing high activity of prolyl endopeptidase are susceptible to activation-induced cell death. FEBS Lett. 2002 Feb 13;512(1-3):163-7. [Content Brief]
[3]. Di Daniel E, et al. Prolyl oligopeptidase binds to GAP-43 and functions without its peptidase activity. Mol Cell Neurosci. 2009 Jul;41(3):373-82. [Content Brief]
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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