PEPA

Hersteller MedChem Express
Kategorie
Typ Inhibitors
Specific against other
Menge 5mg
ArtNr HY-12509-5mg
Eclass 6.1 30220300
Eclass 9.0 32160605
Lieferbar
CAS
141286-78-4
MWt
402.436
Formula
C16H16F2N2O4S2
Solubility
10 mM in DMSO
Clinical_Information
No Development Reported
Pathway
Membrane Transporter/Ion Channel, Neuronal Signaling
Target
iGluR, iGluR
Biological Activity
PEPA is an allosteric modulator of AMPA receptors, binds to the GluA2o and GluA3o LBDs and can be utilized as an indicator of AMPA receptor heterogeneity.
IC50 value:
Target: AMPAR modulator
in vitro: PEPA dose-dependently potentiated AMPA-induced increase of [Ca2+]i. In 90% (72 out of 80) of the cells in which cyclothiazide acts, PEPA potentiated the increased [Ca2+]i induced by AMPA with pronounced cell-to-cell variation in rat hippocampal cultures [1]. PEPA bound to the binding domains of the GluA2 and GluA3 flop isoforms of AMPA receptors [2]. coapplication of AMPA with PEPA protected hippocampal CA1 neurons from brain ischemia-induced death. Coapplication of AMPA with PEPA could prevent downregulated expression of GluR2 subunit caused by ischemia and increase BDNF expression via Lyn-ERK1/2-CREB signaling [4].
in vivo: PEPA (3, 10, 30mg/kg body weight) or vehicle was intraperitoneally administered into stressed mice once before the first extinction session. The significant decrease of the freezing response in the extinction sessions was only seen in the 30mg/kg PEPA-administered stressed mice, compared with vehicle-administered stressed mice [3].
Menge: 5mg
Lieferbar: In stock
Listenpreis: 143,21 €
Rabatt: -10,0%
Preis: 128,89 €
Sie sparen: 14,32 €
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