| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Morphiceptin primarily targets the μ-opioid receptor, a part of the opioid receptor system in the body that plays a crucial role in pain perception. It exhibits an affinity for μ receptors that is at least 1000 times greater than its affinity for enkephalin (δ) receptors. This high specificity makes it a valuable tool for studying μ-opioid receptor function.
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|---|---|
| ln Vitro |
In vitro, Morphiceptin demonstrates potent agonist activity at the μ-opioid receptor. In bioassays using the guinea pig ileum, it demonstrates agonist activity with a potency comparable to morphine. It shows significantly reduced activity in the mouse vas deferens preparation, confirming its selectivity for μ over δ receptors.
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| ln Vivo |
Morphiceptin significantly inhibits the binding of [3H]dihydromorphine, 125I-labeled FK33824 and [3H]naloxone to rat meningeal preparations with a 50% inhibitory concentration (IC50) of approximately 20 nM [1].
In vivo, Morphiceptin has morphinelike activities and is highly specific for morphine (μ) receptors. It is used to investigate the physiological functions and biochemical properties of opiate receptor subtypes, particularly the μ-opioid receptor. Its resistance to peptidase degradation makes it a useful tool for in vivo studies. |
| Enzyme Assay |
μ-Opioid receptor binding is assessed using radioligand binding assays. Membrane preparations from cells expressing the human μ-opioid receptor are incubated with varying concentrations of Morphiceptin and a radiolabeled antagonist. Nonspecific binding is determined in the presence of an excess of unlabeled ligand, and the Ki value is calculated from competitive binding curves.
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| Cell Assay |
Functional activity is assessed in cells expressing the μ-opioid receptor. The compound's ability to stimulate G-protein activation or inhibit cAMP accumulation is measured. A dose-response curve is generated, and the EC50 is calculated.
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| Animal Protocol |
In vivo activity is evaluated in animal models of pain, such as the tail-flick or hot-plate tests. Morphiceptin is administered via various routes, and its analgesic effect is measured. Its potency and duration of action are compared to those of morphine and other opioids.
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| ADME/Pharmacokinetics |
As a peptide, Morphiceptin is expected to have poor oral bioavailability and a short half-life due to rapid proteolytic degradation. However, its resistance to peptidase degradation may provide some advantage over other peptides. It is typically administered via injection in research settings.
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| Toxicity/Toxicokinetics |
As a μ-opioid receptor agonist, Morphiceptin may cause side effects similar to morphine, including respiratory depression, constipation, and the potential for tolerance and dependence. However, its high selectivity for μ receptors may reduce some side effects associated with other opioid receptors.
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| References | |
| Additional Infomation |
Morphin peptide is an oligopeptide.
Morphiceptin is a research compound used to investigate the physiological functions and biochemical properties of opiate receptor subtypes, particularly the μ-opioid receptor. Its high specificity and resistance to peptidase degradation make it a valuable tool for studying opioid pharmacology. It was first isolated from rat brain in 1982. |
| Molecular Formula |
C28H35N5O5
|
|---|---|
| Molecular Weight |
521.61
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| Exact Mass |
521.264
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| CAS # |
74135-04-9
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| PubChem CID |
119303
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| Appearance |
White to off-white solid powder
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| Density |
1.327±0.06 g/cm3(Predicted)
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| Boiling Point |
919.9±65.0 °C(Predicted)
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| LogP |
2.124
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
38
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| Complexity |
855
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| Defined Atom Stereocenter Count |
4
|
| SMILES |
C1C[C@H](N(C1)C(=O)[C@H](CC2=CC=C(C=C2)O)N)C(=O)N[C@@H](CC3=CC=CC=C3)C(=O)N4CCC[C@H]4C(=O)N
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| InChi Key |
LSQXZIUREIDSHZ-ZJZGAYNASA-N
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| InChi Code |
InChI=1S/C28H35N5O5/c29-21(16-19-10-12-20(34)13-11-19)27(37)33-15-5-9-24(33)26(36)31-22(17-18-6-2-1-3-7-18)28(38)32-14-4-8-23(32)25(30)35/h1-3,6-7,10-13,21-24,34H,4-5,8-9,14-17,29H2,(H2,30,35)(H,31,36)/t21-,22-,23-,24-/m0/s1
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| Chemical Name |
(2S)-1-[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]-N-[(2S)-1-[(2S)-2-carbamoylpyrrolidin-1-yl]-1-oxo-3-phenylpropan-2-yl]pyrrolidine-2-carboxamide
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| Synonyms |
Tyr-pro-phe-pro amide; Deproceptin; Morphiceptin
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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 : ≥ 250 mg/mL (~479.29 mM)
DMSO : ~125 mg/mL (~239.64 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.99 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.99 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (3.99 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (191.71 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9171 mL | 9.5857 mL | 19.1714 mL | |
| 5 mM | 0.3834 mL | 1.9171 mL | 3.8343 mL | |
| 10 mM | 0.1917 mL | 0.9586 mL | 1.9171 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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