| Size | Price | |
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| Other Sizes |
| Targets |
ERK1 ERK2 MMP-2 MMP-9
Opioid receptors (primarily kappa-opioid receptor, KOR). beta-Neo-Endorphin is an endogenous opioid peptide that acts as an agonist at kappa-opioid receptors, producing potent analgesic effects. It also has affinity for micro- and delta-opioid receptors, but its primary effects are mediated through KOR. |
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| ln Vitro |
β-Neo-Endorphin (0-20 μM, 20 h) enhances wound healing in human keratinocytes[2]. β-Neo-Endorphin (promotes wound healing by activation of the Erk1/2 signaling pathway in human keratinocytes[2]. -Neo-Endorphin (0-20 μM, 12 h) increases keratinocyte migration through activation of metalloproteinase (MMP)-2 and -9[2]. β-Neo-Endorphin (12 h) promotes migration in the fibroblast[2].
beta-Neo-Endorphin is an endogenous opioid peptide that acts as an agonist at kappa-opioid receptors. It has been found to have potent analgesic effects. It is a hypothalamic “big” Leu-enkephalin of porcine origin. The peptide contains nine amino acid residues and is derived from the prodynorphin precursor. Specific in vitro binding affinities (Ki) are not provided; however, as a KOR agonist, it is expected to have sub-nM to low nM affinity. |
| ln Vivo |
beta-Neo-Endorphin has been found to have potent analgesic effects in animal models of pain (e.g., tail-flick, hot-plate tests). It acts as a natural painkiller and has been studied for its potential therapeutic applications in various medical fields. As an endogenous peptide, it is rapidly degraded in vivo, limiting its direct therapeutic utility. No clinical development has occurred.
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| Enzyme Assay |
Cell-free kappa-opioid receptor binding assays are performed using membranes from CHO-K1 cells expressing human kappa-opioid receptors or from guinea pig brain membranes. Membranes are incubated with a kappa-selective radioligand (e.g., [3H]-U69,593, 0.5-2 nM) and increasing concentrations of beta-Neo-Endorphin (0.001-10,000 nM) in 50 mM Tris-HCl (pH 7.4) containing 1 mM EDTA, 5 mM MgCl2, and 0.1% BSA for 60-90 min at 25degC. Bound radioactivity is separated by GF/B filtration. Ki values are calculated by nonlinear regression using the Cheng-Prusoff equation. For micro and delta assays, [3H]-DAMGO and [3H]-DPDPE are used, respectively.
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: Human keratinocytes (HaCaT) Tested Concentrations: 0, 5, 10 and 20 μM Incubation Duration: 20 h Experimental Results: Dramatically increased the wound closure. Had no observable effect on cell viability. Western Blot Analysis[2] Cell Types: Human keratinocytes (HaCaT) Tested Concentrations: 0, 5, 10 and 20 μM Incubation Duration: 12 h Experimental Results: Activated Erk1/2, phosphorylated P90RSK and Elk-1, demonstrated significant upregulation of MMP-2 and -9 expression. Cells expressing kappa-opioid receptors (e.g., CHO-K1 cells stably expressing KOR) are loaded with a cAMP detection kit (HTRF). beta-Neo-Endorphin is added at increasing concentrations (0.01-10,000 nM) to the cells, and inhibition of forskolin-stimulated cAMP accumulation is measured. EC50 for KOR activation is determined from dose-response curves. For calcium mobilization assays, cells loaded with Fluo-4 AM are used. Alternatively, primary cultures of dorsal root ganglion (DRG) neurons can be used to assess KOR-mediated inhibition of calcium channel currents or neuronal excitability using electrophysiology. |
| Animal Protocol |
For in vivo studies, beta-Neo-Endorphin is dissolved in sterile saline or artificial CSF. Due to poor BBB penetration, it is typically administered by intracerebroventricular (i.c.v.) or intrathecal (i.t.) injection. For analgesic studies, mice or rats are injected i.c.v. (1-20 ug/animal) or i.t. (0.5-10 ug/animal). Analgesia is assessed by the tail-flick test (radiant heat) or hot-plate test at 5, 10, 15, 30, and 60 min post-injection. Antinociceptive responses are expressed as percentage of maximum possible effect (%MPE). Reversal studies using the kappa-selective antagonist nor-binaltorphimine (nor-BNI) are performed to confirm KOR-mediated effects. For PK studies, beta-Neo-Endorphin is administered i.v. to rodents, and plasma and brain samples are collected for LC-MS/MS analysis.
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| ADME/Pharmacokinetics |
No specific PK data are reported for beta-Neo-Endorphin. The molecular weight is 1100.27 (C54H77N13O12). CAS 77739-21-0. The compound is a nonapeptide. It is not orally bioavailable and has a very short plasma half-life (minutes) due to rapid degradation by peptidases (aminopeptidases, endopeptidases). For in vivo studies, it is administered centrally (i.c.v., i.t.) to circumvent BBB issues. Solubility: water 90 mg/mL (ultrasonic). Storage: -20degC, protect from light, dry, sealed. Peptide stability is improved by formulation in sterile saline and immediate use.
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| Toxicity/Toxicokinetics |
No toxicity data are reported for beta-Neo-Endorphin. As an endogenous peptide, it is generally considered safe at physiological concentrations. At doses used in research (i.c.v. up to 20 ug/animal), no signs of toxicity (seizures, respiratory depression, or mortality) have been reported. The compound is not intended for clinical use. No FDA approval. For research use only.
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| References |
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| Additional Infomation |
beta-Neo-endorphin is a derivative of α-neoendorphin with a C-terminal deletion.
Other information: beta-Neo-Endorphin (CAS 77739-21-0) is a research-grade peptide, not FDA-approved. It is an endogenous nonapeptide opioid derived from prodynorphin, belonging to the dynorphin/neoendorphin family. It acts as a kappa-opioid receptor agonist with potent analgesic effects. It is a valuable tool for studying KOR-mediated pain modulation and the endogenous opioid system. Synonyms: beta-Neoendorphin, beta-NEP. For research use only. |
| Molecular Formula |
C54H77N13O12
|
|---|---|
| Molecular Weight |
1100.27
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| Exact Mass |
1099.58
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| CAS # |
77739-21-0
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| PubChem CID |
122260
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Index of Refraction |
1.653
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| LogP |
1.59
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| Hydrogen Bond Donor Count |
14
|
| Hydrogen Bond Acceptor Count |
15
|
| Rotatable Bond Count |
32
|
| Heavy Atom Count |
79
|
| Complexity |
2020
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| Defined Atom Stereocenter Count |
7
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| SMILES |
CC(C)C[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC1=CC=C(C=C1)O)C(=O)N2CCC[C@H]2C(=O)O)NC(=O)[C@H](CC3=CC=CC=C3)NC(=O)CNC(=O)CNC(=O)[C@H](CC4=CC=C(C=C4)O)N
|
| InChi Key |
RTXIYIQLESPXIV-VLOLPVCOSA-N
|
| InChi Code |
InChI=1S/C54H77N13O12/c1-32(2)26-41(65-51(76)42(28-33-10-4-3-5-11-33)62-46(71)31-60-45(70)30-61-47(72)38(56)27-34-15-19-36(68)20-16-34)50(75)64-40(13-8-24-59-54(57)58)48(73)63-39(12-6-7-23-55)49(74)66-43(29-35-17-21-37(69)22-18-35)52(77)67-25-9-14-44(67)53(78)79/h3-5,10-11,15-22,32,38-44,68-69H,6-9,12-14,23-31,55-56H2,1-2H3,(H,60,70)(H,61,72)(H,62,71)(H,63,73)(H,64,75)(H,65,76)(H,66,74)(H,78,79)(H4,57,58,59)/t38-,39-,40-,41-,42-,43-,44-/m0/s1
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| Chemical Name |
(2S)-1-[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[2-[[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]acetyl]amino]acetyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]hexanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]pyrrolidine-2-carboxylic acid
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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) |
H2O: 100 mg/mL (90.89 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.9089 mL | 4.5443 mL | 9.0887 mL | |
| 5 mM | 0.1818 mL | 0.9089 mL | 1.8177 mL | |
| 10 mM | 0.0909 mL | 0.4544 mL | 0.9089 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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