PeptideDB

Pep2m, myristoylated TFA (Myr-Pep2m TFA)

Pep2m, myristoylated TFA (Myr-Pep2m TFA)

CAS No.:

Pep2m, myristoylated TFA (Myr-Pep2m TFA) is a cell-permeable (penetrable) peptide. Pep2m, myristoylated TFA, disrupts th
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This product is for research use only, not for human use. We do not sell to patients.

Pep2m, myristoylated TFA (Myr-Pep2m TFA) is a cell-permeable (penetrable) peptide. Pep2m, myristoylated TFA, disrupts the protein kinase ζ (PKMζ) downstream target NSF/GluR2 interaction. PKMζ A PKC isoenzyme with autonomous activity.

Physicochemical Properties


Molecular Formula C65H119F3N18O16S
Molecular Weight 1497.83
Related CAS # Pep2m, myristoylated;1423381-07-0
Appearance White to off-white solid powder
HS Tariff Code 2934.99.9001
Storage

Powder-20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity


Targets NSF/GluR2 interactions[1]
ln Vitro Pep2m, myristoylated TFA (10 μM), inhibits AMPA receptor (AMPAR) potentiation mediated by PKMζ[1]. Myristoylated TFA, Pep2m, and LTP maintenance do not prevent the rise of PKMζ in hippocampus slices, suggesting that preventing NSF/GluR2 connections does not stop PKMζ synthesis from being induced[1]. Pep2m, myristoylated TFA, reverses persistent potentiation at both weakly stimulated and powerfully stimulated synapses that undergo synaptic tagging and capture, and prevents NSF/GluR2-mediated AMPAR trafficking [1].
ln Vivo In the formalin test, paw withdrawal thresholds (PWTs) on nociceptive responses increase in response to Pep2m, myristoylated TFA (10 µg/20 µL)[2].
Animal Protocol Animal/Disease Models: Female and male Long-Evans hooded rats (8 weeks)[2 ]
Doses: 10 µg (in 20 µL)
Route of Administration: Intrathecal injection
Experimental Results: Resulted in an increase in PWTs, in both male and female rats at various time points tested.
References

[1]. PKMζ Maintains Late Long-Term Potentiation by N-Ethylmaleimide-Sensitive Factor/GluR2-Dependent Trafficking of Postsynaptic AMPA Receptors. J Neurosci. 2008 Jul 30; 28(31): 7820-7827.

[2]. Sex differences in the contributions of spinal atypical PKCs and downstream targets to the maintenance of nociceptive sensitization. Mol Pain. 2019; 15: 1744806919840582.


Solubility Data


Solubility (In Vitro) DMSO :~33.33 mg/mL (~22.25 mM)
H2O :~3.33 mg/mL (~2.22 mM)
Solubility (In Vivo) Solubility in Formulation 1: ≥ 2.5 mg/mL (1.67 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (1.67 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 0.6676 mL 3.3382 mL 6.6763 mL
5 mM 0.1335 mL 0.6676 mL 1.3353 mL
10 mM 0.0668 mL 0.3338 mL 0.6676 mL
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.