| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
micro-opioid receptor (MOR). Dermorphin exhibits >1700-fold selectivity for MOR over delta-opioid receptors, with minimal cross-reactivity at kappa-opioid receptors.
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| ln Vitro |
Dermomorphine is the peptide receptor (NOP) component of the endogenous agonist nociceptin/orphanin FQ (N/OFQ), which is derived from the skin of the leaf jellyfish frog. Dermorphin and DeNo displace [3H]-DPN binding in CHOhMu displacement binding experiments in a concentration-dependent and saturable way. At the delta receptor, dermorphin exhibited an affinity of 7.17, whereas N/OFQ was unable to displace [3H]-DPN. Dermorphin and DeNo induce a concentration-dependent and saturable binding of GTPγ[35S] to Mu receptors [2].
In vitro, dermorphin stimulates concentration-dependent and saturable binding of GTPgamma[3⁵S] at the micro-opioid receptor. It is approximately 30-fold more potent than the standard MOR agonist DAMGO in electrophysiological assays, with an effective dose range of 0.05-5 pmol. Dermorphin shows high binding affinity with a Ki of 0.54 nM and Kd of 1.24 nM at MOR. |
| ln Vivo |
In vivo, dermorphin produces potent analgesic effects through highly selective activation of MOR. It has been shown to suppress neuropathic pain in animal models. The peptide exhibits rapid onset and stronger analgesic action compared to morphine.
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| Enzyme Assay |
Receptor binding assays are performed using membrane preparations from cells expressing recombinant micro-opioid receptors. Membranes are incubated with radiolabeled [3H]-dermorphin or [3H]-DAMGO in binding buffer at 25degC for 60-90 minutes. Non-specific binding is determined in the presence of excess unlabeled naloxone (10 microM). Bound and free ligand are separated by rapid filtration through GF/B glass fiber filters, followed by scintillation counting. Competitive binding curves are generated using increasing concentrations of unlabeled dermorphin to calculate Ki values. GTPgamma[3⁵S] binding assays are conducted to evaluate receptor activation, where membranes are incubated with GDP, GTPgamma[3⁵S], and varying concentrations of dermorphin, and bound radioactivity is quantified.
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| Cell Assay |
Dermorphin activity is assessed in cells stably or transiently expressing MOR. Cells are seeded in 96-well plates and treated with increasing concentrations of dermorphin (0.01 nM to 10 microM) for 15-30 minutes. Receptor activation is measured by quantifying cAMP accumulation (inhibition of forskolin-stimulated cAMP production) using ELISA or HTRF-based kits. Alternatively, MOR-mediated G-protein activation is evaluated by [3⁵S]GTPgammaS binding in cell membrane preparations. Calcium mobilization assays or beta-arrestin recruitment assays can also be employed to assess downstream signaling. EC₅0 values are calculated from dose-response curves using nonlinear regression analysis.
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| Animal Protocol |
Analgesic efficacy is evaluated in rodent models such as the tail-flick test or hot-plate test. Mice or rats are administered dermorphin via intracerebroventricular (ICV), intrathecal (IT), or subcutaneous routes at doses ranging from 0.05-5 pmol (ICV) or higher for systemic administration. Pain threshold is measured at multiple time points post-administration (e.g., 5, 15, 30, 60 minutes). Antinociceptive effect is expressed as percentage of maximal possible effect (%MPE). The opioid receptor specificity of the analgesic response is confirmed by pre-administration of the opioid antagonist naloxone. Neuropathic pain models, such as chronic constriction injury (CCI) or spinal nerve ligation (SNL), are also used to evaluate dermorphin's efficacy in inhibiting neuropathic pain behaviors.
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| ADME/Pharmacokinetics |
Dermorphin exhibits rapid brain penetration due to its peptide nature when administered centrally. Systemic bioavailability is limited by peptide degradation and poor oral absorption. The peptide has a relatively short plasma half-life (typically minutes) due to proteolytic cleavage, though the D-Ala2 residue confers enhanced metabolic stability compared to all-L peptides. The primary route of elimination is via renal filtration and enzymatic degradation.
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| Toxicity/Toxicokinetics |
Dermorphin is generally well-tolerated at analgesic doses in animal studies. Typical opioid-related adverse effects may include respiratory depression, constipation, tolerance development, and physical dependence with repeated administration. The therapeutic index is favorable due to high MOR selectivity, which reduces off-target effects. No significant organ-specific toxicity has been reported at pharmacological doses. Long-term safety data are limited as dermorphin is primarily a research tool.
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| References |
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| Additional Infomation |
Pimofen is an oligopeptide. Pimofen has reportedly been found in Agalichnis callidryas, and relevant data is available for reference.
Dermorphin is not an approved therapeutic agent; it is strictly a research compound used in opioid pharmacology studies. The peptide serves as a valuable tool for studying MOR structure-activity relationships, opioid receptor signaling, and analgesic mechanisms. Its D-alanine at position 2 is a rare feature among animal-derived peptides that contributes to its exceptional potency and enzymatic stability. Dermorphin analogs are being investigated for potential pain management applications with reduced side-effect profiles. The compound is available as a lyophilized powder with ≥98% purity for research purposes only. |
| Molecular Formula |
C40H50N8O10
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|---|---|
| Molecular Weight |
802.872609615326
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| Exact Mass |
802.365
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| CAS # |
77614-16-5
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| Related CAS # |
Dermorphin TFA;78331-26-7
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| PubChem CID |
5485199
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| Appearance |
White to off-white solid powder
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| LogP |
3.986
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| Hydrogen Bond Donor Count |
10
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
19
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| Heavy Atom Count |
58
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| Complexity |
1410
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| Defined Atom Stereocenter Count |
6
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| SMILES |
C[C@H](C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)NCC(=O)N[C@@H](CC2=CC=C(C=C2)O)C(=O)N3CCC[C@H]3C(=O)N[C@@H](CO)C(=O)N)NC(=O)[C@H](CC4=CC=C(C=C4)O)N
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| InChi Key |
FHZPGIUBXYVUOY-VWGYHWLBSA-N
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| InChi Code |
InChI=1S/C40H50N8O10/c1-23(44-37(55)29(41)18-25-9-13-27(50)14-10-25)36(54)46-30(19-24-6-3-2-4-7-24)38(56)43-21-34(52)45-31(20-26-11-15-28(51)16-12-26)40(58)48-17-5-8-33(48)39(57)47-32(22-49)35(42)53/h2-4,6-7,9-16,23,29-33,49-51H,5,8,17-22,41H2,1H3,(H2,42,53)(H,43,56)(H,44,55)(H,45,52)(H,46,54)(H,47,57)/t23-,29+,30+,31+,32+,33+/m1/s1
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| Chemical Name |
(2S)-N-[(2S)-1-amino-3-hydroxy-1-oxopropan-2-yl]-1-[(2S)-2-[[2-[[(2S)-2-[[(2R)-2-[[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]propanoyl]amino]-3-phenylpropanoyl]amino]acetyl]amino]-3-(4-hydroxyphenyl)propanoyl]pyrrolidine-2-carboxamide
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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) |
H2O : ~120 mg/mL (~149.46 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (124.55 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.1246 mL | 0.6228 mL | 1.2455 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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