PeptideDB

Dynorphin A (1-10) (TFA)

Dynorphin A (1-10) (TFA)

CAS No.:

Dynorphin A (1-10) (TFA) is an endogenous opioid neuropeptide that binds to the κ-opioid receptor. Dynorphin A (1-10) (
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Dynorphin A (1-10) (TFA) is an endogenous opioid neuropeptide that binds to the κ-opioid receptor. Dynorphin A (1-10) (TFA) also blocks NMDA-activated currents with IC50 of 42.0 μM.

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
*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.