| 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 |
gamma1-MSH targets the melanocortin-3 receptor (MC3R) with high affinity. It has a Ki of 34 nM for rat MC3 receptors and a Ki of 1318 nM for MC4 receptors. The pKi for MC3 is 7.46. MC3R is a G-protein coupled receptor involved in the regulation of energy homeostasis, sodium balance, and blood pressure.
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| ln Vitro |
In vitro, gamma1-MSH binds selectively to MC3 receptors with approximately 40-fold selectivity over MC4. It activates MC3R and downstream signaling pathways, including cAMP accumulation. The peptide's activity at MC3R makes it a valuable tool for studying the role of MC3 in sodium balance and blood pressure regulation.
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| ln Vivo |
In vivo, gamma1-MSH increases the release of extracellular dopamine, which induces grooming and vertical activity (rearing) in rats. It exhibits hypertensive effects and regulates sodium balance. These effects are mediated through activation of MC3R in the central nervous system.
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| Enzyme Assay |
Receptor binding assays for gamma1-MSH use membrane preparations from cells expressing MC3 or MC4 receptors. Radiolabeled MSH is incubated with varying concentrations of the test peptide, and binding affinity (Ki) is determined from competition binding curves.
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| Cell Assay |
Cellular assays for gamma1-MSH typically use cell lines expressing melanocortin receptors. Cells are treated with the peptide, and cAMP accumulation is measured as a readout of receptor activation. Selectivity for MC3 over MC4 is confirmed in these assays.
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| Animal Protocol |
In vivo studies with gamma1-MSH are conducted in rodent models. The peptide is typically administered via intracerebroventricular (ICV) or intraperitoneal injection. Behavioral assays for grooming and rearing are performed. Blood pressure and sodium balance are also monitored.
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| ADME/Pharmacokinetics |
As a peptide, gamma1-MSH is expected to have a short half-life due to proteolytic degradation. The compound should be stored at -20degC. Standard peptide handling and storage procedures apply.
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| Toxicity/Toxicokinetics |
Toxicity data for gamma1-MSH are limited. Peptide hormones are generally well-tolerated at physiological concentrations. Standard safety precautions for laboratory handling of peptides should be followed.
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| References | |
| Additional Infomation |
γ-MSH is an 11-amino acid peptide derived from the N-terminal fragment of proopiomelanotropinogen (POMC). γ-MSH can stimulate adrenal steroid production and plays a regulatory role in the cardiovascular and renal systems.
gamma1-MSH is a research-use peptide and is not approved for therapeutic applications. It is also known as Gamma1-MSH. The peptide is derived from the ACTH/beta-lipotropin precursor protein and is used to study melanocortin receptor pharmacology, sodium balance, and blood pressure regulation. It is available from multiple research suppliers. |
| Molecular Formula |
C72H97N21O14S
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|---|---|
| Molecular Weight |
1512.73788
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| Exact Mass |
1511.72
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| CAS # |
72629-65-3
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| PubChem CID |
57339641
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| Appearance |
White to off-white solid powder
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| LogP |
5.503
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| Hydrogen Bond Donor Count |
22
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| Hydrogen Bond Acceptor Count |
19
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| Rotatable Bond Count |
47
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| Heavy Atom Count |
108
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| Complexity |
2990
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| Defined Atom Stereocenter Count |
10
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| SMILES |
CC(C)[C@@H](C(=O)N[C@@H](CCSC)C(=O)NCC(=O)N[C@@H](CC1=CNC=N1)C(=O)N[C@@H](CC2=CC=CC=C2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC3=CNC4=CC=CC=C43)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC5=CC=CC=C5)C(=O)N)NC(=O)[C@H](CC6=CC=C(C=C6)O)N
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| InChi Key |
SLEIICTWQFRIFM-SLNSXFHGSA-N
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| InChi Code |
InChI=1S/C72H97N21O14S/c1-40(2)60(93-62(99)48(73)30-43-22-24-46(94)25-23-43)70(107)88-52(26-29-108-3)63(100)83-38-58(95)85-56(34-45-37-79-39-84-45)68(105)90-54(32-42-16-8-5-9-17-42)66(103)86-51(21-13-28-81-72(77)78)65(102)91-55(33-44-36-82-49-19-11-10-18-47(44)49)67(104)92-57(35-59(96)97)69(106)87-50(20-12-27-80-71(75)76)64(101)89-53(61(74)98)31-41-14-6-4-7-15-41/h4-11,14-19,22-25,36-37,39-40,48,50-57,60,82,94H,12-13,20-21,26-35,38,73H2,1-3H3,(H2,74,98)(H,79,84)(H,83,100)(H,85,95)(H,86,103)(H,87,106)(H,88,107)(H,89,101)(H,90,105)(H,91,102)(H,92,104)(H,93,99)(H,96,97)(H4,75,76,80)(H4,77,78,81)/t48-,50-,51-,52-,53-,54-,55-,56-,57-,60-/m0/s1
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| Chemical Name |
(3S)-3-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylbutanoyl]amino]-4-methylsulfanylbutanoyl]amino]acetyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-3-phenylpropanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-4-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-oxobutanoic 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, 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 0.6611 mL | 3.3053 mL | 6.6105 mL | |
| 5 mM | 0.1322 mL | 0.6611 mL | 1.3221 mL | |
| 10 mM | 0.0661 mL | 0.3305 mL | 0.6611 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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