| 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 |
Melanocortin-4 receptor (MC4-R)[1]
Melanocortin-4 receptor (MC4-R), a G protein-coupled receptor (GPCR) primarily expressed in the central nervous system, is the primary molecular target. beta-MSH is an endogenous agonist for MC4-R, which regulates energy homeostasis, appetite, and body weight. The peptide also exhibits high affinity at MC3-R and may have activity at other melanocortin receptors. |
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| ln Vitro |
Human β-MSH (beta-melanocyte stimulating hormone) exhibits strong affinity for human MC4-R transfected into CHO cells (Ki = 11.4±0.4 nM) as well as MC4-R in rat hypothalamus homogenates (Ki = 5.0±0.4 nM)[1].
In cell-free radioligand binding assays, beta-MSH (human) binds to human MC4-R transfected into CHO cells with a Ki value of 11.4 +/- 0.4 nM. It also binds to MC4-R in rat hypothalamic homogenates with a Ki value of 5.0 +/- 0.4 nM. Activation of MC4-R by beta-MSH stimulates cAMP production through Gs protein coupling, which can be measured in cell-based functional assays. |
| ln Vivo |
In vivo, beta-MSH is an endogenous neuropeptide that regulates appetite and energy balance via MC4-R activation. Intracerebroventricular (ICV) administration of beta-MSH in rodents suppresses food intake and reduces body weight. It also plays roles in pigmentation (via MC1-R in melanocytes), sexual function, and the stress response through the hypothalamic-pituitary-adrenal axis.
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| Enzyme Assay |
For competitive binding assays, membranes from MC4-R-expressing cells (CHO or HEK293) are incubated with a radiolabeled tracer (e.g., [¹2⁵I]-NDP-MSH) and varying concentrations of unlabeled beta-MSH (0.001-1000 nM) in binding buffer (25 mM HEPES pH 7.4, 1 mM CaCl2, 5 mM MgCl2, 0.5% BSA) at 25degC for 60-120 minutes. Bound radioligand is separated by filtration and quantified by gamma counting. Ki values are calculated by nonlinear regression.
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| Cell Assay |
For cellular functional assays, cells expressing MC4-R (e.g., HEK293-MC4R) are seeded in 96-well plates and treated with beta-MSH (0.001-1000 nM) in assay buffer containing a cAMP bioluminescence resonance energy transfer (BRET) or HTRF detection reagent. The increase in cAMP levels is measured after 15-30 minutes of stimulation. EC50 values are typically in the low nanomolar range.
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| Animal Protocol |
For in vivo studies, beta-MSH (0.1-10 nmol) is administered by intracerebroventricular (ICV) injection into the lateral ventricle of fasting mice or rats. Food intake is measured at 1, 2, 4, and 24 hours post-injection. Body weight change and metabolic parameters (e.g., oxygen consumption, energy expenditure) can also be assessed in metabolic cages. The MC4-R antagonist SHU9119 can be used as a control to confirm receptor specificity.
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| ADME/Pharmacokinetics |
PK properties of beta-MSH: As a 22-amino acid peptide, it has a very short plasma half-life (minutes) due to rapid proteolytic degradation. It is not orally bioavailable. The TFA salt is formulated for research use as a lyophilized powder, which is reconstituted in water or dilute acetic acid to a stock concentration (0.1-1 mM) and stored at -80degC. Avoid repeated freeze-thaw cycles.
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| Toxicity/Toxicokinetics |
Toxicity of beta-MSH is low at typical experimental doses (nmol range). No significant toxicity has been reported. The peptide is for research use only and not for human or veterinary therapeutic applications. Standard peptide handling precautions (avoid inhalation, use gloves) should be observed.
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| References |
[1]. Harrold JA, et al. beta-MSH: a functional ligand that regulated energy homeostasis via hypothalamic MC4-R? Peptides. 2003 Mar;24(3):397-405.
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| Additional Infomation |
beta-Melanocyte Stimulating Hormone (beta-MSH) is part of the pro-opiomelanocortin (POMC) family of peptides, which also includes alpha-MSH, gamma-MSH, and ACTH. The human beta-MSH sequence is different from rodent beta-MSH, and species selectivity should be considered when extrapolating results. The TFA salt is used to improve solubility and stability for in vitro and ex vivo studies. This product is for research use only.
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| Molecular Formula |
C120H175F3N34O37S
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|---|---|
| Molecular Weight |
2774.94
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| Related CAS # |
β-Melanocyte Stimulating Hormone (MSH), human;17908-57-5
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| Appearance |
Typically exists as solid at room temperature
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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 (~36.04 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 | 0.3604 mL | 1.8018 mL | 3.6037 mL | |
| 5 mM | 0.0721 mL | 0.3604 mL | 0.7207 mL | |
| 10 mM | 0.0360 mL | 0.1802 mL | 0.3604 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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