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 |