PEPA
- Product Name
- PEPA
- CAS No.
- 141286-78-4
- Chemical Name
- PEPA
- Synonyms
- PEPA;PEPA;PEPA, 10 mM in DMSO;PEPA,inhibit,Inhibitor,iGluR,Ionotropic glutamate receptors;2-[2,6-Difluoro-4-[[2-[(phenylsulfonyl)amino]ethyl]thio]phenoxy]acetamide;Acetamide, 2-[2,6-difluoro-4-[[2-[(phenylsulfonyl)amino]ethyl]thio]phenoxy]-;2,6-Difluoro-4-[2-(phenylsul-fonyl-amino)-ethyl-thio]-phenoxy-acet-amide (PEPA)
- CBNumber
- CB0972925
- Molecular Formula
- C16H16F2N2O4S2
- Formula Weight
- 402.44
- MOL File
- 141286-78-4.mol
PEPA Property
- Boiling point:
- 617.6±65.0 °C(Predicted)
- Density
- 1.47±0.1 g/cm3(Predicted)
- storage temp.
- protect from light
- solubility
- DMSO: >20mg/mL
- form
- solid
- pka
- 10.44±0.40(Predicted)
- color
- white
- InChI
- InChI=1S/C16H16F2N2O4S2/c17-13-8-11(9-14(18)16(13)24-10-15(19)21)25-7-6-20-26(22,23)12-4-2-1-3-5-12/h1-5,8-9,20H,6-7,10H2,(H2,19,21)
- InChIKey
- GTACSIONMHMRPD-UHFFFAOYSA-N
- SMILES
- C(N)(=O)COC1=C(F)C=C(SCCNS(C2=CC=CC=C2)(=O)=O)C=C1F
Safety
- WGK Germany
- 3
N-Bromosuccinimide Price
- Product number
- D8941
- Product name
- 2,6-Difluoro-4-[2-(phenylsulfonylamino)ethylthio]phenoxyacetamide
- Purity
- ≥98% (HPLC), solid
- Packaging
- 5mg
- Price
- $183
- Updated
- 2025/07/31
- Product number
- D8941
- Product name
- 2,6-Difluoro-4-[2-(phenylsulfonylamino)ethylthio]phenoxyacetamide
- Purity
- ≥98% (HPLC), solid
- Packaging
- 25mg
- Price
- $748
- Updated
- 2025/07/31
- Product number
- 29190
- Product name
- PEPA
- Packaging
- 5mg
- Price
- $88
- Updated
- 2024/03/01
- Product number
- 29190
- Product name
- PEPA
- Packaging
- 10mg
- Price
- $121
- Updated
- 2024/03/01
- Product number
- P999023
- Product name
- PEPA
- Packaging
- 25mg
- Price
- $190
- Updated
- 2021/12/16
PEPA Chemical Properties,Usage,Production
Description
PEPA is a positive allosteric modulator (PAM) of AMPA receptors. It selectively increases glutamate-induced currents in X. laevis oocytes expressing the flop isoforms of the AMPA receptor subunits glutamate receptor 3 (GluR3) and GluR4 over the flip isoforms of these subunits at 200 μM. PEPA (10 mg/kg) decreases the latency to find the platform in the Morris water maze, indicating reversal of memory deficits, in a rat model of memory impairment induced by middle cerebral artery occlusion (MCAO). It decreases freezing time in a contextual fear freezing paradigm in mice when administered at a dose of 30 mg/kg.
Uses
PEPA is an allosteric potentiator of AMPA desensitization.
Biological Activity
Novel allosteric potentiator of AMPA receptor desensitization. Slows the rate of onset of desensitization and potentiates steady-state equilibrium currents induced by glutamate with subunit (GluR3/4 > GluR1) and splice variant (flop > flip) selectivity. Ameliorates post-ischemic memory impairment in rats following i.v. administration.
Biochem/physiol Actions
2,6-Difluoro-4-[2-(phenylsul-fonyl-amino)-ethyl-thio]-phenoxy-acet-amide is a structurally novel, selective, high affinity AMPA ionotropic glutamate receptor agonist that reduces ischemia-induced performance deficits in rats.
in vivo
PEPA (30 mg/kg; i.p.; once) decreases freezing time in a contextual fear freezing paradigm in mice[3].
| Animal Model: | Male C57BL/6J mice (10-12 weeks old) were applied stress (a 2 h restraint, a 20 min forced swim, and ether inhalation)[3] |
| Dosage: | 3 mg/kg, 10 mg/kg, 30 mg/kg |
| Administration: | i.p.; once |
| Result: | The significant decrease of the freezing response in the extinction sessions was only seen in the 30 mg/kg. |
References
[1] Sekiguchi, M., Fleck, M.W., Mayer, M.L., et al. A novel allosteric potentiator of AMPA receptors: 4-[2-(phenylsulfonylamino)ethylthio]-2,6-difluoro-phenoxyacetamide. J. Neurosci. 17(15), 5760-5771 (1997).
[2] Sekiguchi, M., Yamada, K., Jin, J., et al. The AMPA receptor allosteric potentiator PEPA ameliorates post-ischemic memory impairment. Neuroreport 12(13), 2947-29950 (2001).
[3] KO ZUSHIDA. Facilitation of extinction learning for contextual fear memory by PEPA: a potentiator of AMPA receptors.[J]. Journal of Neuroscience, 2007, 27 1: 158-166. DOI:10.1523/JNEUROSCI.3842-06.2007.
PEPA Preparation Products And Raw materials
Raw materials
Preparation Products
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