| 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 |
δ Opioid Receptor/DOR μ Opioid Receptor/MOR
beta-Endorphin targets micro-opioid receptors (MOR) and delta-opioid receptors (DOR), both of which are G protein-coupled receptors (GPCRs) involved in pain modulation, reward, and stress responses. It binds with high affinity to both receptor subtypes, with Ki values typically in the low nanomolar range (e.g., Ki = 0.1-1 nM for MOR). Activation of these receptors inhibits adenylyl cyclase and reduces neuronal excitability. |
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| ln Vitro |
The release of dopamine in the striatum is inhibited by β-enddorphin and equine TFA at 0, 0.6, 1.2, and 3 μM [4].
In cell-free radioligand binding assays, equine beta-endorphin binds to micro- and delta-opioid receptors with high affinity. The peptide activates G protein signaling as measured by [3⁵S]GTPgammaS binding assays, with EC50 values in the low nanomolar range. It is a full agonist at both receptor subtypes, producing maximal stimulation comparable to other opioid agonists such as DAMGO (for MOR). |
| ln Vivo |
In rats, β-endorphin and equine TFA (2 or 20 μg/kg; intraperitoneally once) influence acquisition and retention.
In vivo, beta-endorphin, equine TFA exhibits potent analgesic (pain-relieving) properties in animal models. When administered centrally (intracerebroventricular or intrathecal), it produces dose-dependent antinociception in tail-flick, hot plate, and formalin tests. It also plays roles in reward, stress adaptation, and regulation of neuroendocrine function, similar to other endogenous opioid peptides. |
| Enzyme Assay |
For receptor binding assays, membranes from cells expressing micro- or delta-opioid receptors (e.g., CHO-micro, CHO-delta) are incubated with a radiolabeled opioid antagonist (e.g., [3H]-diprenorphine or [3H]-naloxone, 0.5-2 nM) and varying concentrations of beta-endorphin (0.001-1000 nM) in binding buffer (50 mM Tris-HCl pH 7.4, 5 mM MgCl2, 0.1% BSA) at 25degC for 60-90 minutes. Nonspecific binding is determined with 10 uM naloxone. Bound radioligand is separated by filtration and quantified by scintillation counting.
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| Cell Assay |
For functional assays, cells expressing opioid receptors are seeded in 96-well plates and stimulated with beta-endorphin (0.001-1000 nM) in assay buffer. Receptor activation is measured by a cAMP HTRF or BRET biosensor (decrease in cAMP levels) or by a [3⁵S]GTPgammaS binding assay (increase in G protein activation). EC50 values for beta-endorphin are typically in the low nanomolar range (1-10 nM).
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| Animal Protocol |
Animal/Disease Models: Adult Female Wistar rats[3]
Doses: 2 or 20 μg/kg Route of Administration: 2 or 20 μg/kg; ip, once Experimental Results: Hindered the acquisition of shuttle avoidance learning and habituation of a rearing response to a tone at a dose of 20 μg/kg. Caused amnesia in the avoidance task with the pre- or post-training administration of 2 μg/kg and pre-training administration of 20 μg/kg. For in vivo analgesic studies, beta-endorphin (0.1-10 nmol) is administered by intracerebroventricular (ICV) injection or intrathecal (IT) injection into mice or rats. Antinociception is measured 15-60 minutes post-injection using the tail-flick test (thermal stimulus), hot plate test, or acetic acid-induced writhing test (chemical stimulus). The opioid antagonist naloxone (1-5 mg/kg, IP) is co-administered to confirm receptor-specific effects. |
| ADME/Pharmacokinetics |
PK properties of beta-endorphin: As a 31-amino acid peptide, it has a very short half-life (minutes) in plasma due to rapid proteolytic degradation by peptidases. It is not orally bioavailable. The TFA salt is a lyophilized powder that is reconstituted in water, saline, or dilute acetic acid (0.1-1 mM stock) and stored at -80degC. Working solutions are prepared fresh in saline or PBS.
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| Toxicity/Toxicokinetics |
Toxicity of beta-endorphin is low at typical experimental doses (nmol range). No significant toxicity has been reported in laboratory animals at analgesic doses. High doses may cause respiratory depression, as with other opioid agonists. Standard peptide handling precautions (avoid inhalation, use gloves) should be observed. Not for human use.
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| References |
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| Additional Infomation |
beta-Endorphin, equine TFA is a valuable research tool for studying opioid receptor signaling, pain mechanisms, addiction, and neuroendocrine regulation. The equine sequence is used for comparative studies across species. The TFA salt form improves solubility and stability, facilitating use in receptor binding, functional assays, and in vivo behavioral studies. This product is for research use only and is not for diagnostic or therapeutic applications.
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| Molecular Formula |
C156H249F3N42O46S
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| Molecular Weight |
3537.96
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| Related CAS # |
β-Endorphin, equine;79495-86-6
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| Appearance |
White to off-white solid powder
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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 :~100 mg/mL (~28.26 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 | 0.2826 mL | 1.4132 mL | 2.8265 mL | |
| 5 mM | 0.0565 mL | 0.2826 mL | 0.5653 mL | |
| 10 mM | 0.0283 mL | 0.1413 mL | 0.2826 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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