Dermorphin
Based on 1 publication(s) in Google Scholar
Dermorphin is a natural heptapeptide μ-opioid receptor (MOR) agonist found in amphibian skin. Inhibition of neuropathic pain.
For research use only. We do not sell to patients.
- Purity: 99.36%
- CAS No.: 77614-16-5
- Formula: C40H50N8O10
- Molecular Weight:802.87
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Storage:
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)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Dermorphin
MoreAll Opioid Receptor Isoforms
More
Biological Activity
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μ Opioid Receptor/MOR |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
0.72 nM
Compound: dermorphin
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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
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[PMID: 19621878] |
| CHO | IC50 |
197 nM
Compound: dermorphin
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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
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[PMID: 19621878] |
| HEK293 | IC50 |
>10000 nM
Compound: dermorphin
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Displacement of [3H]NOC from human ORL1 receptor expressed in HEK293 cells
Displacement of [3H]NOC from human ORL1 receptor expressed in HEK293 cells
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[PMID: 16814543] |
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.
Chemical Information
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CAS No. 77614-16-5
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Appearance Solid
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Molecular Weight 802.87
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Formula C40H50N8O10
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Color White to off-white
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Sequence
Tyr-{d-Ala}-Phe-Gly-Tyr-Pro-Ser-NH2
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Sequence Shortening
Y-{d-Ala}-FGYPS-NH2
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Structure Classification
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Initial Source
skin of the frog Phyllomedusa sauvagei
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
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)
Publications (1)
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Journal Impact Factor
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Most Recent
Solvent & Solubility
H2O : ≥ 100 mg/mL (124.55 mM)
* "≥" means soluble, but saturation unknown.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (124.55 mM); Clear solution; Need ultrasonic
Protocol
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
[1]. Tiwari V, et al. Activation of Peripheral μ-opioid Receptors by Dermorphin [D-Arg2, Lys4] (1-4) Amide Leads to Modality-preferred Inhibition of Neuropathic Pain. Anesthesiology. 2016 Mar;124(3):706-20. [Content Brief]
[2]. Bird MF, et al. Characterisation of the Novel Mixed Mu-NOP Peptide Ligand Dermorphin-N/OFQ (DeNo). PLoS One. 2016 Jun 7;11(6):e0156897. [Content Brief]
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.
Dermorphin Related Classifications
HY-P0244 Related Classifications
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