2. GPCR/G Protein Neuronal Signaling Metabolic Enzyme/Protease
  3. Opioid Receptor Endogenous Metabolite
  4. Dynorphin A (1-8)

Dynorphin A (1-8) is a ligand with preference for the κ-opioid receptor, and its IC50 value against human placental κ-opioid receptor is 330 nM. Dynorphin A (1-8) mediates neuroprotective effects by inhibiting oxidative stress, suppressing apoptosis, and competitively displacing the binding of κ partial agonists. Dynorphin A (1-8) is the dominant opioid peptide in human placental villi and tissue extracts; it undergoes rapid hydrolysis and can enter the central nervous system via intranasal administration. Dynorphin A (1-8) can be used in studies related to ischemic stroke.

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Dynorphin A (1-8)

Dynorphin A (1-8) Chemical Structure

CAS No. : 75790-53-3

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Based on 1 publication(s) in Google Scholar

Dynorphin A (1-8) Related Antibodies

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Human Endogenous Metabolite Microbial Metabolite

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Description

Dynorphin A (1-8) is a ligand with preference for the κ-opioid receptor, and its IC50 value against human placental κ-opioid receptor is 330 nM. Dynorphin A (1-8) mediates neuroprotective effects by inhibiting oxidative stress, suppressing apoptosis, and competitively displacing the binding of κ partial agonists. Dynorphin A (1-8) is the dominant opioid peptide in human placental villi and tissue extracts; it undergoes rapid hydrolysis and can enter the central nervous system via intranasal administration. Dynorphin A (1-8) can be used in studies related to ischemic stroke[1][2][3].

IC50 & Target

κ Opioid Receptor/KOR

 

Human Endogenous Metabolite

 

In Vitro

Dynorphin A (1-8) inhibits 3H-EKC binding to the purified 63 kDa kappa opioid receptor from human placental villus tissue with an IC50 of 330 nM[2].
Dynorphin A (1-8) inhibits 3H-Bremazocine binding to the purified 63 kDa kappa opioid receptor from human placental villus tissue with an IC50 of 610 nM and a Ki of 303 nM[2].

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

Dynorphin A (1-8) Related Antibodies
In Vivo

Dynorphin A (1-8) (100 nmol (0.098 mg); intranasal; single dose at start of surgery) provides significant neuroprotection in MCAO rats by reducing neurological deficits, cerebral infarction volume, brain edema, neuronal apoptosis, and oxidative stress, while Dynorphin A (1-8) (100 nmol; intravenous; single dose at start of surgery) shows no significant therapeutic effect[1].

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

Animal Model: Sprague-Dawley (SD) (male, 240-270 g, middle cerebral artery occlusion modeling)[1]
Dosage: 100 nmol (intranasal, neuroprotective); 100 nmol (intravenous, no effect)
Administration: intranasal; single dose at start of surgery; intravenous; single dose at start of surgery
Result: Significantly reduced neurological deficit scores.
Significantly reduced cerebral infarction volume.
Significantly reduced brain water content.
Increased neuron number, improved cell arrangement, and reduced neuronal degeneration, necrosis, and pyknosis.
Significantly reduced the number of TUNEL-positive apoptotic neurons.
Significantly increased Bcl-2 expression and decreased Bax and Caspase-3 expression in the ischemic cortex.
Significantly increased serum SOD activity and decreased serum MDA concentration.
Showed no statistically significant effects on neurological deficit scores, cerebral infarction volume, brain water content, TUNEL-positive neuron count, or apoptosis-related protein expression compared to the MCAO model group.
Molecular Weight

981.15

Formula

C46H72N14O10
CAS No.
Appearance

Solid

Color

White to off-white

Sequence

Tyr-Gly-Gly-Phe-Leu-Arg-Arg-Ile
Sequence Shortening

YGGFLRRI
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Stored under nitrogen, away from moisture

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : 100 mg/mL (101.92 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.0192 mL 5.0961 mL 10.1921 mL
5 mM 0.2038 mL 1.0192 mL 2.0384 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 (stored under nitrogen, away from moisture). 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.

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  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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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: 99.88%

SDS (254 KB)

COA (247 KB) LCMS (92 KB) Elemental Analysis Report (106 KB)

Handling Instructions (2659 KB)
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 (stored under nitrogen, away from moisture). 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
H2O 1 mM 1.0192 mL 5.0961 mL 10.1921 mL 25.4803 mL
5 mM 0.2038 mL 1.0192 mL 2.0384 mL 5.0961 mL
10 mM 0.1019 mL 0.5096 mL 1.0192 mL 2.5480 mL
15 mM 0.0679 mL 0.3397 mL 0.6795 mL 1.6987 mL
20 mM 0.0510 mL 0.2548 mL 0.5096 mL 1.2740 mL
25 mM 0.0408 mL 0.2038 mL 0.4077 mL 1.0192 mL
30 mM 0.0340 mL 0.1699 mL 0.3397 mL 0.8493 mL
40 mM 0.0255 mL 0.1274 mL 0.2548 mL 0.6370 mL
50 mM 0.0204 mL 0.1019 mL 0.2038 mL 0.5096 mL
60 mM 0.0170 mL 0.0849 mL 0.1699 mL 0.4247 mL
80 mM 0.0127 mL 0.0637 mL 0.1274 mL 0.3185 mL
100 mM 0.0102 mL 0.0510 mL 0.1019 mL 0.2548 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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Dynorphin A (1-8) Related Classifications

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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.

Keywords:

Dynorphin A (1-8)75790-53-3Opioid ReceptorEndogenous Metaboliteoxidative stressNMDA receptorhuman placental villusMCAO ratshuman placental κ-opioid receptorapoptosisischemic strokeneuroprotective effectscentral nervous systemκ-opioid receptorInhibitorinhibitorinhibit

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