| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
μ Opioid Receptor/MOR 1.11 nM (Ki)
Endomorphin 1 acetate targets the μ-opioid receptor as a selective, high-affinity agonist with a Ki of 1.11 nM. It also has high affinity for the kappa3 binding site with Ki values between 20 and 30 nM. The μ-opioid receptor is the primary target for endogenous opioid peptides and is involved in pain modulation, reward, and other physiological processes. By activating μ-opioid receptors, Endomorphin 1 acetate produces potent antinociceptive and analgesic effects. Its selectivity and high affinity make it a valuable tool for studying μ-opioid receptor function. |
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| ln Vitro |
With a pIC50 value of 8.03 in CHOμ cells, endomorphin 1 acetate suppresses the production of cyclic AMP induced by forskolin (1 μM)[5]. In Caco-2 cells, endomorphin 1 (1–10 μM) acetate stimulates the release of interleukin-8[6]. Adult rat substantia gelatinosa neurons exhibit excitatory transmission inhibition upon exposure to 1 μM acetate of endomorphin 1[7].
In vitro, Endomorphin 1 acetate is a selective, high-affinity μ-opioid receptor agonist with a Ki of 1.11 nM. When CACO-2 cells were treated with various concentrations of Endomorphin 1 acetate alone, no changes in basal IL-8 production were detected. However, in the presence of IL-1β, treatment significantly increased IL-8 production compared to IL-1β alone. The compound's high affinity for μ-opioid receptors and kappa3 binding sites makes it a valuable research tool. |
| ln Vivo |
Endomorphin 1 (icv) acetate has an ED50 value of 6.16 nM in mice, indicating antinociceptive characteristics[2]. By suppressing the inflammatory response, endomorphin 1 (50 μg/kg, IV, rats) acetate reduces myocardial ischemia/reperfusion injury (MIRI)[3].
In vivo, Endomorphin 1 acetate (50 μg/kg, i.v.) was studied in male Sprague Dawley rats subjected to myocardial ischemia-reperfusion injury. In IR, IPO, and Endomorphin 1 acetate groups, LDH and CK-MB activities were significantly higher than control. Compared to the IR group, LDH and CK-MB activities were significantly lower in IPO and Endomorphin 1 acetate groups. IL-6 and TNF-α levels were significantly elevated in the IR group compared to control, and were significantly reduced in IPO and Endomorphin 1 acetate groups compared to IR. These findings demonstrate cardioprotective and anti-inflammatory effects. |
| Enzyme Assay |
For μ-opioid receptor binding assays, membrane preparations from cells expressing recombinant μ-opioid receptors are incubated with radiolabeled ligands and varying concentrations of Endomorphin 1 acetate. Non-specific binding is determined using excess unlabeled reference compounds (e.g., naloxone). Following incubation at appropriate temperature (typically 25°C for 60-90 minutes), bound and free radioligands are separated by rapid filtration through glass fiber filters. Filters are washed and radioactivity counted by liquid scintillation. Ki values (1.11 nM) are calculated from competition curves. For functional assays, G protein activation is measured by [35S]-GTPγS binding.
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| Cell Assay |
For in vitro cellular assays, cell lines expressing μ-opioid receptors or CACO-2 cells are cultured in appropriate media under standard conditions (37°C, 5% CO2). Endomorphin 1 acetate is dissolved in DMSO or appropriate buffer and diluted in culture medium to desired concentrations. Cells are treated with compound for specified durations. Receptor activation is assessed by measuring downstream signaling (e.g., cAMP inhibition). For cytokine studies, IL-8 production is measured by ELISA. Cell viability can be assessed using standard assays. Each concentration is tested in replicate wells with vehicle controls.
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| Animal Protocol |
Animal/Disease Models: ICR mice[2].
Doses: 6.16 nM (ED50) Route of Administration: Intracerebroventricularly (icv) injection Experimental Results: Inhibited dose-dependently the tail-flick response. Animal/Disease Models: Rats[3]. Doses: 50 μg/kg Route of Administration: intravenously (iv) following LAD ligation for 25 min, subsequently the LAD was reperfused for 120 min. Experimental Results: Alleviated MIRI by reducing the production of free radicals. Dncreased LDH and CK-MB activities. Increased SOD activity and diminished MDA content. diminished IL-6 and TNF-α plasma content. For in vivo animal studies, Endomorphin 1 acetate is typically formulated in suitable vehicles and administered via intravenous (i.v.) injection. In myocardial ischemia-reperfusion injury studies, male Sprague Dawley rats underwent LAD ligation (30 minutes ischemia) followed by 120 minutes reperfusion. Endomorphin 1 acetate (50 μg/kg) was administered intravenously 25 minutes after LAD ligation. Cardiac injury markers (LDH, CK-MB) and inflammatory cytokines (IL-6, TNF-α) were measured. All procedures must follow institutional animal care and use committee guidelines. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of Endomorphin 1 acetate are characteristic of a peptide. The compound has a molecular weight of 670.75, formula C36H42N6O7, and CAS number 1276123-71-7. Purity: 99.74%. Appearance: white solid. Storage: typically at -20°C for powder; in solvent at -80°C. Solubility: DMSO 90 mg/mL. As a peptide, it is typically administered parenterally and may have limited oral bioavailability and short half-life due to proteolytic degradation. Specific pharmacokinetic parameters are reported in the primary literature.
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| Toxicity/Toxicokinetics |
According to available safety information, Endomorphin 1 acetate is intended for research purposes only and is not for human use. Standard laboratory safety precautions should be followed when handling this compound, including the use of appropriate personal protective equipment (gloves, lab coat, safety goggles). The compound should be handled in a well-ventilated area. Avoid dust formation and inhalation. In case of skin contact, wash with plenty of soap and water. In case of eye contact, rinse cautiously with water for several minutes. No clinical toxicity data are available.
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| References |
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| Additional Infomation |
Endomorphin 1 acetate is a selective, high-affinity μ-opioid receptor agonist with a Ki of 1.11 nM. It also has high affinity for kappa3 (Ki 20-30 nM). It has antinociceptive and analgesic effects and is used to study neurological diseases. At 50 μg/kg i.v., it shows cardioprotective and anti-inflammatory effects in ischemia-reperfusion models. It has a molecular weight of 670.75 and formula C36H42N6O7. It is for research use only with no regulatory approvals reported.
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| Molecular Formula |
C36H42N6O7
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|---|---|
| Molecular Weight |
670.754688739777
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| Exact Mass |
670.311
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| CAS # |
1276123-71-7
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| Related CAS # |
Endomorphin 1;189388-22-5
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| PubChem CID |
165437298
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
7
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
12
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| Heavy Atom Count |
49
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| Complexity |
1060
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| Defined Atom Stereocenter Count |
4
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| SMILES |
CC(=O)O.C1C[C@H](N(C1)C(=O)[C@H](CC2=CC=C(C=C2)O)N)C(=O)N[C@@H](CC3=CNC4=CC=CC=C43)C(=O)N[C@@H](CC5=CC=CC=C5)C(=O)N
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| InChi Key |
ISCQEYDGKZTCMS-YAOJAVRNSA-N
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| InChi Code |
InChI=1S/C34H38N6O5.C2H4O2/c35-26(17-22-12-14-24(41)15-13-22)34(45)40-16-6-11-30(40)33(44)39-29(19-23-20-37-27-10-5-4-9-25(23)27)32(43)38-28(31(36)42)18-21-7-2-1-3-8-21;1-2(3)4/h1-5,7-10,12-15,20,26,28-30,37,41H,6,11,16-19,35H2,(H2,36,42)(H,38,43)(H,39,44);1H3,(H,3,4)/t26-,28-,29-,30-;/m0./s1
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| Chemical Name |
acetic acid;(2S)-1-[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]-N-[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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: 125 mg/mL (186.36 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.10 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 (3.10 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 (3.10 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 | 1.4909 mL | 7.4543 mL | 14.9087 mL | |
| 5 mM | 0.2982 mL | 1.4909 mL | 2.9817 mL | |
| 10 mM | 0.1491 mL | 0.7454 mL | 1.4909 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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