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My Cart> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > Membrane Transporter & Ion Channel > PEPACAS：141286-78-4
Molecular Formula：C16H16F2N2O4S2
Molecular Weight：402.44
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to off-white Solid
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| CAS | 141286-78-4 |
| Name | PEPA |
| Molecular Formula | C16H16F2N2O4S2 |
| Molecular Weight | 402.44 |
| Solubility | Soluble in DMSO(Need ultrasonic) |
| Purity | ≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD04974493 |
| SMILES | C1=CC=C(C=C1)S(=O)(=O)NCCSC2=CC(=C(C(=C2)F)OCC(=O)N)F |
| InChIKey | GTACSIONMHMRPD-UHFFFAOYSA-N |
| 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) |
| PubChem CID | 6603828 |
| Target Point | iGluR |
| Passage | Membrane Transporter&Ion Channel |
| Background | PEPA is an AMPAR allosteric regulator that can bind the LBDs domain of GluA2o/GluA3o. |
| Biological Activity | PEPA 是 AMPA 受体的异构调节剂，能与 GluA2o 和 GluA3o LBD 结合。[1-3] |
| In Vitro | PEPA dose-dependently potentiated AMPA-induced increase of [Ca2+]. In Xenopus oocytes，the potentiation of AMPA response by PEPA varied with subunit and splice-variant combinations，and the P/C ratio was between 0.19 and 2.20.[1] Coapplication of AMPA with PEPA protected hippocampal CA1 neurons from brain ischemia-induced death. TrkB receptor-mediated PI3K/Akt signal pathway was activated after coapplication of AMPA with PEPA，and protected CA1 neurons against ischemic insults through depression of JNK3 activity.[3] |
| In Vivo | PEPA facilitates extinction of contextual fear in stressed mice. The significant decrease of the freezing response in the extinction sessions was seen in the PEPA(30mg/kg，intraperitoneally administered)stressed mice.[2] |
| Data Literature Source | [1]. Sekiguchi M，et al. Pharmacological detection of AMPA receptor heterogeneity by use of two allosteric potentiators in rat hippocampal cultures. Br J Pharmacol. 1998 Apr;123(7):1294-303. [2]. Yamada D，et al. Facilitating actions of an AMPA receptor potentiator upon extinction of contextually conditioned fear response in stressed mice. Neurosci Lett. 2011 Jan 25;488(3):242-6. [3]. Zhang QG，ET AL. Positive modulation of AMPA receptors prevents downregulation of GluR2 expression and activates the Lyn-ERK1/2-CREB signaling in rat brain ischemia. Hippocampus. 2010 Jan;20(1):65-77. |
| Unit | Bottle |
| Specification | 5mg |
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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