1. GPCR/G Protein Neuronal Signaling
  2. Opioid Receptor
  3. Dermorphin

Dermorphin is a natural heptapeptide μ-opioid receptor (MOR) agonist found in amphibian skin. Inhibition of neuropathic pain.

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Synthèse de peptides personnalisée

Dermorphin

Dermorphin Chemical Structure

CAS No. : 77614-16-5

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10 mg En stock
25 mg En stock
50 mg En stock
100 mg   Obtenir un devis  
200 mg   Obtenir un devis  

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Other Forms of Dermorphin:

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Description

Dermorphin is a natural heptapeptide μ-opioid receptor (MOR) agonist found in amphibian skin. Inhibition of neuropathic pain[1].

IC50 & Target

μ Opioid Receptor/MOR

 

Cellular Effect
Cell Line Type Value Description References
CHO IC50
0.72 nM
Compound: dermorphin
Displacement of [3H]DAMGO from mu opioid receptor expressed in CHO cells after 90 mins by scintillation counting
Displacement of [3H]DAMGO from mu opioid receptor expressed in CHO cells after 90 mins by scintillation counting
[PMID: 19621878]
CHO IC50
197 nM
Compound: dermorphin
Displacement of [3H]DPDPE from delta opioid receptor expressed in CHO cells after 90 mins by scintillation counting
Displacement of [3H]DPDPE from delta opioid receptor expressed in CHO cells after 90 mins by scintillation counting
[PMID: 19621878]
HEK293 IC50
>10000 nM
Compound: dermorphin
Displacement of [3H]NOC from human ORL1 receptor expressed in HEK293 cells
Displacement of [3H]NOC from human ORL1 receptor expressed in HEK293 cells
[PMID: 16814543]
HEK293 IC50
>10 μM
Compound: dermorphin
Displacement of [3H]NOC from human ORL1 receptor expressed in HEK293 cells
Displacement of [3H]NOC from human ORL1 receptor expressed in HEK293 cells
[PMID: 16814543]
In Vitro

Dermorphin, a peptide isolated from the skin of Phyllomedusa frogs and the peptide receptor (NOP) component by the endogenous agonist nociceptin/orphanin FQ (N/OFQ). In displacement binding studies at CHOhMu, Dermorphin and DeNo displac the binding of [3H]-DPN in a concentration dependent and saturable manner. Dermorphin displays an affinity of 7.17, while N/OFQ fails to displace [3H]-DPN at the Delta receptor. Dermorphin and DeNo stimulate the binding of GTPγ[35S] in a concentration dependent and saturable manner at the Mu receptor[2].

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

Masse moléculaire

802.87

Formule

C40H50N8O10

CAS No.
Appearance

Solid

Color

White to off-white

Sequence

Tyr-{d-Ala}-Phe-Gly-Tyr-Pro-Ser-NH2

Sequence Shortening

Y-{d-Ala}-FGYPS-NH2

Structure Classification
Initial Source

skin of the frog Phyllomedusa sauvagei

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

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

Solvant et solubilité
In Vitro: 

H2O : ≥ 100 mg/mL (124.55 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.2455 mL 6.2277 mL 12.4553 mL
5 mM 0.2491 mL 1.2455 mL 2.4911 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). 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.

  • Calculateur de molarité

  • Calculateur de dilution

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  PBS

    Solubility: 100 mg/mL (124.55 mM); Clear solution; Need ultrasonic

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).
Pureté et documentation

Purity: 99.36%

Références
Essai de kinase
[2]

Membrane protein (40 μg) is incubated in 0.5 mL volume of 50 mM Tris, 0.2 mM EGTA, 1 mM MgCl2, 100 mM NaCl, 0.1% BSA, 0.15 mM bacitracin; pH 7.4, GDP (33 μM), and ∼150 pM GTPγ[35S]. Varying concentrations of reference ligands (Dermorphin, N/OFQ, Dynorphin-A and Leu-enkephalin) or DeNo (1 pM-10 μM) is added prior to incubation. Non-specific binding is determined in the presence of unlabeled GTPγS (10 μM). Samples are incubated at 30°C for 1 h with gentle agitation. Reactions are terminated by vacuum filtration through dry Whatman GF/B filters, using a Brandel harvester[2].

MCE n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement.

Références

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). 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 1.2455 mL 6.2277 mL 12.4553 mL 31.1383 mL
5 mM 0.2491 mL 1.2455 mL 2.4911 mL 6.2277 mL
10 mM 0.1246 mL 0.6228 mL 1.2455 mL 3.1138 mL
15 mM 0.0830 mL 0.4152 mL 0.8304 mL 2.0759 mL
20 mM 0.0623 mL 0.3114 mL 0.6228 mL 1.5569 mL
25 mM 0.0498 mL 0.2491 mL 0.4982 mL 1.2455 mL
30 mM 0.0415 mL 0.2076 mL 0.4152 mL 1.0379 mL
40 mM 0.0311 mL 0.1557 mL 0.3114 mL 0.7785 mL
50 mM 0.0249 mL 0.1246 mL 0.2491 mL 0.6228 mL
60 mM 0.0208 mL 0.1038 mL 0.2076 mL 0.5190 mL
80 mM 0.0156 mL 0.0778 mL 0.1557 mL 0.3892 mL
100 mM 0.0125 mL 0.0623 mL 0.1246 mL 0.3114 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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Nom du produit:
Dermorphin
Cat. No.:
HY-P0244
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