Pep2m
Pep2m is a peptide receptor inhibitor. Pep2m inhibits the interaction between the C-terminus of the AMPA-type glutamate receptor (GluA2) subunit and N-ethylmaleimide-sensitive fusion protein (NSF). Pep2m prevents synaptic long-term depression (LTD). Pep2m can reduce postsynaptic currents in neurons, AMPA-mediated currents in cultured hippocampal neurons, and AMPA receptor surface expression[1][2][3][4][5].
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- No. CAS: 243843-42-7
- Fòrmula: C49H92N18O13S
- Peso molecular:1173.43
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Actividad biológica
Descripciòn
IC50 & Target
[1][2][3][4][5]|
AMPA Receptor |
In Vitro
Pep2m reduces EPSC amplitude and blocks LTD in CA1 pyramidal cells of hippocampal slices by reducing the number of functional AMPARs[1].
Pep2m reduces the current response to locally applied AMPA in cultured hippocampal neurons[2].
Pep2m reduces the frequency of recorded AMPA-miniature excitatory postsynaptic currents (mEPSCs) in the presence of tetrodotoxin (TTX)[2].
Pep2m reduces the surface expression of AMPA receptors containing AMPA-type glutamate receptors (GluR2), but does not reduce the surface expression of NMDA receptors and the ingrowth aggregation of AMPA receptors[2].
Pep2m does not affect basal synaptic transmission and low-frequency stimulation (LFS)-induced LTD in young GluA2 KO mice, and does not affect basal synaptic transmission but restores LFS-induced LTD in mature GluA2 KO mice[3].
Pep2m reduces AMPA-induced radiolabeled norepinephrine ([3H]NA) but not AMPA-induced radiolabeled acetylcholine ([3H]Ach) release[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult male C57B6J mice (8 weeks) [4]
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Dosage:1 μL of 450 nM
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Administration:ICV, once
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Result:Impaired learning rate and long-term memory expression.
Chemical Information
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No. CAS 243843-42-7
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Peso molecular 1173.43
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Fòrmula C49H92N18O13S
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Sequence
Lys-Arg-Met-Lys-Val-Ala-Lys-Asn-Ala-Gln
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Sequence Shortening
KRMKVAKNAQ
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[1]. Lüthi A, et al.Hippocampal LTD expression involves a pool of AMPARs regulated by the NSF-GluR2 interaction. Neuron. 1999 Oct;24(2):389-99. [Content Brief]
[2]. Noel J, et al.Surface expression of AMPA receptors in hippocampal neurons is regulated by an NSF-dependent mechanism. Neuron. 1999 Jun;23(2):365-76. [Content Brief]
[3]. Cao F, et al. Hippocampal Long-Term Depression in the Presence of Calcium-Permeable AMPA Receptors. Front Synaptic Neurosci. 2018 Nov 13;10:41. [Content Brief]
[4]. Conboy L, et al. Stress at learning facilitates memory formation by regulating AMPA receptor trafficking through a glucocorticoid action. Neuropsychopharmacology. 2010 Feb;35(3):674-85. [Content Brief]
[5]. Pittaluga A, et al. Trafficking of presynaptic AMPA receptors mediating neurotransmitter release: neuronal selectivity and relationships with sensitivity to cyclothiazide. Neuropharmacology. 2006 Mar;50(3):286-96. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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