| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Adrenorphin targets the micro-opioid receptor (MOR), a G protein-coupled receptor that mediates the analgesic and euphoric effects of endogenous and exogenous opioids. It acts as a potent agonist at this receptor, with a Ki of 12 nM. The peptide also inhibits nicotine-induced release of adrenaline and noradrenaline, with an IC50 of 10 uM. This activity is more than 100-fold more potent than the reported nicotine-induced inhibition. Adrenorphin is an endogenous ligand that plays a role in modulating pain and stress responses.
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| ln Vitro |
Adrenorphin (Metorphamide) is an opioid octapeptide derived from the brain of cows and a strong agonist of μ-opioid receptors, with a Ki of 12 nM. Ki for the μ-opioid receptor/Ki for the δ-opioid receptor is 0.04, while Ki for the μ-opioid receptor/Ki for the κ-opioid receptor is 0.46[1]. In cultured human pheochromocytoma 6 cells, adrenaline efficiently suppresses 10 μM nicotine-induced catecholamine production with an IC50 of 1.1 μM [2].
In vitro studies have characterized Adrenorphin as a potent micro-opioid receptor agonist with a Ki of 12 nM. It is a potent inhibitor of nicotine-induced adrenaline and noradrenaline release, with an IC50 of 10 uM. The peptide shows higher than 100-fold more potent inhibition of nicotine-induced catecholamine release compared to other reported inhibitors. Its activity as an inhibitor of met5-enkephalin has also been reported. The compound is a valuable tool for studying opioid receptor pharmacology and neuroendocrine regulation. |
| ln Vivo |
In vivo studies of Adrenorphin are limited, as the peptide is primarily used as a research tool for in vitro studies. As an endogenous opioid peptide, it would be expected to have analgesic and neuroendocrine effects in vivo. However, its rapid degradation by proteases would limit its bioavailability and duration of action. The peptide's role in modulating pain and stress responses has been inferred from its in vitro activity and its presence in the adrenal medulla. Specific in vivo efficacy data are not extensively reported.
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| Enzyme Assay |
The in vitro receptor binding assay for Adrenorphin involves competitive binding studies using membrane preparations from cells expressing the micro-opioid receptor. Radiolabeled opioid ligands (e.g., [3H]-DAMGO) are used as tracers. Varying concentrations of Adrenorphin are incubated with the membrane preparation and the radioligand. Bound radioactivity is measured after filtration. The Ki value of 12 nM is determined from competition curves. Data are analyzed using nonlinear regression models. Selectivity is confirmed by testing against other opioid receptor subtypes (delta and kappa).
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| Cell Assay |
In vitro cellular assays for Adrenorphin are conducted using cells expressing the micro-opioid receptor, such as CHO or HEK293 cells transfected with MOR. Cells are treated with varying concentrations of Adrenorphin. Receptor activation is assessed by measuring the inhibition of forskolin-stimulated cAMP accumulation or by measuring G protein activation using [35S]GTPgammaS binding assays. The EC50 values are determined from dose-response curves. For catecholamine release studies, chromaffin cells or other catecholamine-secreting cells are used, and the inhibition of nicotine-induced release is measured.
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| Animal Protocol |
In vivo animal studies for Adrenorphin are not extensively reported. As an endogenous opioid peptide, it could be evaluated in animal models of pain, stress, or addiction. Typical study designs would involve administration of the peptide via intracerebroventricular or systemic routes, followed by assessment of analgesic effects (e.g., tail-flick or hot-plate tests) or neuroendocrine parameters. However, specific published in vivo protocols for Adrenorphin are not available in the provided sources. The compound is primarily used as an in vitro research tool.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Adrenorphin are not applicable as the compound is a peptide research tool rather than a therapeutic candidate. The peptide has a molecular weight of 984.18 g/mol and a molecular formula of C44H69N15O9S. As a peptide, it would be susceptible to rapid proteolytic degradation and would have poor oral bioavailability. It is not intended for in vivo administration in pharmacokinetic studies. For in vitro use, it is typically dissolved in aqueous buffers or DMSO. The compound is for research use only.
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| Toxicity/Toxicokinetics |
Toxicology data for Adrenorphin are not applicable as the compound is a peptide research tool. The peptide is not administered to animals or humans for therapeutic purposes. Standard safety precautions for handling peptides should be followed. No specific toxicity data are available. The compound is for research use only and is not intended for human therapeutic applications.
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| References | |
| Additional Infomation |
Adrenorphin (metorphamide) is an endogenous opioid octapeptide that acts as a potent agonist of the micro-opioid receptor with a Ki of 12 nM. It is derived from proenkephalin A and is found in the adrenal medulla. The peptide also inhibits nicotine-induced adrenaline and noradrenaline release with an IC50 of 10 uM. It has a molecular weight of 984.18 g/mol and a molecular formula of C44H69N15O9S. Adrenorphin is used as a research tool for studying opioid receptor pharmacology and neuroendocrine regulation.
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| Molecular Formula |
C44H69N15O9S
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|---|---|
| Molecular Weight |
984.178760000001
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| Exact Mass |
983.512
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| CAS # |
88377-68-8
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| PubChem CID |
122176
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| Appearance |
White to off-white solid powder
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| Density |
1.42g/cm3
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| Index of Refraction |
1.656
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| LogP |
3.1
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| Hydrogen Bond Donor Count |
14
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| Hydrogen Bond Acceptor Count |
13
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| Rotatable Bond Count |
31
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| Heavy Atom Count |
69
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| Complexity |
1730
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| Defined Atom Stereocenter Count |
6
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| SMILES |
CC(C)[C@@H](C(=O)N)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC1=CC=CC=C1)NC(=O)CNC(=O)CNC(=O)[C@H](CC2=CC=C(C=C2)O)N
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| InChi Key |
XJOQRTJDYAHKPY-YVWIMRNGSA-N
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| InChi Code |
InChI=1S/C44H69N15O9S/c1-25(2)36(37(46)63)59-41(67)31(12-8-19-52-44(49)50)57-39(65)30(11-7-18-51-43(47)48)56-40(66)32(17-20-69-3)58-42(68)33(22-26-9-5-4-6-10-26)55-35(62)24-53-34(61)23-54-38(64)29(45)21-27-13-15-28(60)16-14-27/h4-6,9-10,13-16,25,29-33,36,60H,7-8,11-12,17-24,45H2,1-3H3,(H2,46,63)(H,53,61)(H,54,64)(H,55,62)(H,56,66)(H,57,65)(H,58,68)(H,59,67)(H4,47,48,51)(H4,49,50,52)/t29-,30-,31+,32-,33-,36-/m0/s1
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| Chemical Name |
(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[2-[[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]acetyl]amino]acetyl]amino]-3-phenylpropanoyl]amino]-4-methylsulfanylbutanoyl]amino]-N-[(2R)-1-[[(2S)-1-amino-3-methyl-1-oxobutan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-5-(diaminomethylideneamino)pentanamide
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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) |
DMSO : ~50 mg/mL (~50.80 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.54 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 25.0 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: ≥ 2.5 mg/mL (2.54 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 25.0 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: ≥ 2.5 mg/mL (2.54 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.0161 mL | 5.0804 mL | 10.1607 mL | |
| 5 mM | 0.2032 mL | 1.0161 mL | 2.0321 mL | |
| 10 mM | 0.1016 mL | 0.5080 mL | 1.0161 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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