Physicochemical Properties
| Molecular Formula | C59H92F3N19O14 |
| Molecular Weight | 1348.48 |
| Related CAS # | Dynorphin A (1-10);79994-24-4 |
| Appearance | 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 | NMDA Receptor κ Opioid Receptor/KOR |
| ln Vitro | The endogenous opioid neuropeptide dysorphin A(1–10)(TFA) attaches to the κ-receptor's transmembrane domain[1]. Using the whole-cell patch recording method, the non-opioid effects of different types of Dynorphin A (DynA) are investigated on N-methyl-D-aspartate (NMDA) receptor channels in isolated rat trigeminal neurons. Every dynorphin that was tested inhibited currents that were triggered by NMDA. There is no dependence on voltage for the blocking effects. For DynA(1-10), the IC50 is 42.0 μM. We investigated the function of DynA(1–10) at various membrane potentials to find out if shorter dynorphins have the same blocking property. As the membrane potentials shifted from -80 to +60 mV, DynA(1–10) blocked INMDA to a similar degree. Therefore, DynA(1-32) and DynA(1-10) both operate on NMDA receptors in a voltage-independent manner, despite having apparent affinities that differ by 160[2]. |
| References |
[1]. Molecular simulation of dynorphin A-(1-10) binding to extracellular loop 2 of the kappa-opioidreceptor. A model for receptor activation. J Med Chem. 1997 Sep 26;40(20):3254-62. [2]. Dynorphin block of N-methyl-D-aspartate channels increases with the peptide length. J Pharmacol Exp Ther. 1998 Mar;284(3):826-31. |
Solubility Data
| Solubility (In Vitro) |
DMSO :~100 mg/mL (~74.16 mM) H2O :~50 mg/mL (~37.08 mM) |
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (1.85 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% 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 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (1.85 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 3: ≥ 2.5 mg/mL (1.85 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 | 0.7416 mL | 3.7079 mL | 7.4158 mL | |
| 5 mM | 0.1483 mL | 0.7416 mL | 1.4832 mL | |
| 10 mM | 0.0742 mL | 0.3708 mL | 0.7416 mL |