| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
NMDA Receptor κ Opioid Receptor/KOR
kappa-opioid receptor (KOR); functions as an agonist. Also blocks NMDA receptor-activated currents as a non-opioid action. |
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| 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].
Dynorphin A (1-10) TFA is a potent agonist at the kappa-opioid receptor (Ki in the low nanomolar range). It also blocks NMDA-activated currents with an IC50 of 42.0 microM (non-opioid action). These non-opioid actions may contribute to dynorphin-induced spinal cord injury and neurotoxicity. |
| ln Vivo |
As an endogenous kappa-opioid receptor agonist, Dynorphin A (1-10) produces analgesic effects in rodent pain models and modulates dopamine release. At higher doses, it produces aversive effects and has been implicated in stress-induced behaviors and neuropsychiatric disorders.
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| Enzyme Assay |
kappa-Opioid receptor binding affinity (Ki) is measured by competitive radioligand binding using [3H]-U69,593 or [3H]-bremazocine and membranes from CHO or HEK293 cells expressing human kappa-opioid receptor. For NMDA receptor blockade, electrophysiology is used.
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| Cell Assay |
Primary cultured neurons (rat trigeminal neurons) are subjected to whole-cell patch clamp recording; NMDA (10-100 microM) is applied in the presence of increasing concentrations of Dynorphin A (1-10) (1-100 microM); NMDA-activated current amplitude is measured.
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| Animal Protocol |
Rats or mice are administered Dynorphin A (1-10) via intracerebroventricular (ICV) injection (1-10 nmol) or intrathecal (IT) injection (0.5-5 nmol). Analgesia is measured by tail-flick test; motor function is assessed by rotarod; neurotoxicity is evaluated by histology of spinal cord.
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| ADME/Pharmacokinetics |
Not applicable; as a peptide, Dynorphin A (1-10) has very poor oral bioavailability and a short plasma half-life (minutes) due to proteolytic degradation. It is typically administered directly into the CNS (ICV, IT) for in vivo experiments.
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| Toxicity/Toxicokinetics |
No toxicity data available; at high doses, dynorphins produce spinal cord injury and paralysis via non-opioid, NMDA receptor-mediated mechanisms. For research use only, not for human administration.
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| References |
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| Additional Infomation |
Dynorphin A (1-10) TFA is a research-grade peptide tool for studying kappa-opioid receptor signaling, pain modulation, NMDA receptor modulation, and dynorphin-mediated neurotoxicity. It has no clinical trial status or marketing approval. For research use only.
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| Molecular Formula |
C59H92F3N19O14
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| Molecular Weight |
1348.48
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| Related CAS # |
Dynorphin A (1-10);79994-24-4
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| Appearance |
Solid powder
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO :~100 mg/mL (~74.16 mM)
H2O :~50 mg/mL (~37.08 mM) |
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| 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. View More
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. |
| 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.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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