1. GPCR/G Protein Neuronal Signaling Apoptosis Metabolic Enzyme/Protease
  2. Opioid Receptor Apoptosis Caspase Endogenous Metabolite
  3. Dynorphin A

Dynorphin A is an endogenous opioid peptide involved in inhibitory neurotransmission in the central nervous system (CNS). Dynorphin A is a highy potent kappa opioid receptor (KOR) agonist, and is also an agonist for other opioid receptors, such as mu (MOR) and delta (DOR). Dynorphin A can induce neuronal death, and can be used in the research of neurological disease.

For research use only. We do not sell to patients.

Dynorphin A Chemical Structure

Dynorphin A Chemical Structure

CAS No. : 80448-90-4

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Based on 1 publication(s) in Google Scholar

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Description

Dynorphin A is an endogenous opioid peptide involved in inhibitory neurotransmission in the central nervous system (CNS). Dynorphin A is a highy potent kappa opioid receptor (KOR) agonist, and is also an agonist for other opioid receptors, such as mu (MOR) and delta (DOR). Dynorphin A can induce neuronal death, and can be used in the research of neurological disease[1][2].

IC50 & Target[3]

Human Endogenous Metabolite

 

Caspase 3

 

κ Opioid Receptor/KOR

 

In Vitro

Dynorphin A (10 μM, 4 h/72 h) increases caspase-3 activity and the level of cytochrome c released from mitochondria in mouse striatal neurons, and induces neuronal death[3].
dynorphin A (33 μM, 4 h) elevates [Ca2+]i and causes a significant loss of neurons[4].
dynorphin A (1 μM) inhibits the release of vasopressin (VP) from the isolated neural lobe[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[3]

Cell Line: Mouse striatal neurons
Concentration: 10 μM
Incubation Time: 0, 24, 48, 72 h
Result: Induced neuronal death (identified by the fragmentation and destruction of the cell body and neurites).
In Vivo

Dynorphin A (intracerebroventricular injection, 1 μg of 2 μL, a single dose) inhibits vasopressin (VP) release in 24 h water-deprived male rats[5].
Dynorphin A (intracerebroventricular injection, 500 pmol/5 μL per day for 4 d) alleviates stress-induced behavioral impairments in ddY mice accompanied by regulation of the 5-HTergic system in the brain[6].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 24 h water-deprived male rats[5]
Dosage: 1 μg of 2 μL
Administration: Intracerebroventricular injection
Result: Inhibited vasopressin (VP) release 30 min upon injection.
Animal Model: Male ddY mice[6]
Dosage: 15, 150, 1500 pmol/5 μL per day for 4 days
Administration: Intracerebroventricular injection
Result: Attenuated the repeated stress-induced escape failures from the shock.
Molecular Weight

2147.48

Formula

C99H155N31O23

CAS No.
Unlabeled CAS

Appearance

Solid

Color

White to off-white

Sequence

Tyr-Gly-Gly-Phe-Leu-Arg-Arg-Ile-Arg-Pro-Lys-Leu-Lys-Trp-Asp-Asn-Gln

Sequence Shortening

YGGFLRRIRPKLKWDNQ

SMILES

O=C([C@H]1N(CCC1)C([C@H](CCCNC(N)=N)NC([C@H]([C@@H](C)CC)NC([C@H](CCCNC(N)=N)NC([C@H](CCCNC(N)=N)NC([C@H](CC(C)C)NC([C@@H](NC(CNC(CNC([C@@H](N)CC2=CC=C(C=C2)O)=O)=O)=O)CC3=CC=CC=C3)=O)=O)=O)=O)=O)=O)N[C@@H](CCCCN)C(N[C@@H](CC(C)C)C(N[C@@H](CCCCN)C(N[C@H](C(N[C@@H](CC(O)=O)C(N[C@@H](CC(N)=O)C(N[C@H](C(O)=O)CCC(N)=O)=O)=O)=O)CC4=CNC5=CC=CC=C45)=O)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Sealed storage, away from moisture and light

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (46.57 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : ≥ 100 mg/mL (46.57 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.4657 mL 2.3283 mL 4.6566 mL
5 mM 0.0931 mL 0.4657 mL 0.9313 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 3 mg/mL (1.40 mM); Clear solution

    This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 3 mg/mL (1.40 mM); Clear solution

    This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 98.59%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 0.4657 mL 2.3283 mL 4.6566 mL 11.6416 mL
5 mM 0.0931 mL 0.4657 mL 0.9313 mL 2.3283 mL
10 mM 0.0466 mL 0.2328 mL 0.4657 mL 1.1642 mL
15 mM 0.0310 mL 0.1552 mL 0.3104 mL 0.7761 mL
20 mM 0.0233 mL 0.1164 mL 0.2328 mL 0.5821 mL
25 mM 0.0186 mL 0.0931 mL 0.1863 mL 0.4657 mL
30 mM 0.0155 mL 0.0776 mL 0.1552 mL 0.3881 mL
40 mM 0.0116 mL 0.0582 mL 0.1164 mL 0.2910 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Dynorphin A
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