| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg | |||
| Other Sizes |
| Targets |
MC1R[1]
Melanocortin 1 receptor (MC1R). MSG606 is a potent human MC1 receptor antagonist with an IC50 of 17 nM. It also acts as a partial agonist at human MC3 and MC5 receptors, with EC50 values of 59 nM and 1300 nM, respectively. This compound demonstrates selectivity for MC1R over MC3R and MC5R, making it a valuable tool for dissecting MC1R-mediated signaling pathways. |
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| ln Vitro |
In vitro, MSG606 exhibits binding affinity for A375 melanoma cells, which endogenously express MC1R. The compound functions as a competitive antagonist at MC1R, blocking the effects of natural ligands. At higher concentrations, it shows partial agonist activity at MC3R and MC5R, as measured by receptor activation assays in transfected cell lines. The compound's peptide nature ensures high specificity for melanocortin receptors without off-target activity.
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| ln Vivo |
In vivo, MSG606 reverses morphine-induced hyperalgesia in female mice, demonstrating a sex-specific effect with no efficacy observed in male animals. This suggests an estrogen-dependent mechanism of action. The compound's neuroprotective properties have been documented in animal models of neurological disorders. MSG606 does not cross the blood-brain barrier efficiently, limiting its central nervous system effects.
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| Enzyme Assay |
Standard cell-free receptor binding assays for MSG606 utilize membrane preparations from cells expressing recombinant human melanocortin receptors. Membranes (10-20 microg protein) are incubated with 0.5-1 nM [¹2⁵I]-NDP-alpha-MSH as radioligand in 50 mM HEPES buffer pH 7.4 containing 1 mM MgCl2, 2 mM CaCl2, and 0.1% BSA for 60-90 minutes at room temperature with varying concentrations of unlabeled MSG606 (0.01-1000 nM). Non-specific binding is determined in the presence of 1 microM unlabeled NDP-alpha-MSH. Bound radioligand is separated by rapid filtration through GF/B filters presoaked in 0.5% polyethyleneimine, followed by three washes with ice-cold buffer. Filter-bound radioactivity is measured, and IC50 values are calculated by nonlinear regression using the Cheng-Prusoff equation.
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| Cell Assay |
For functional cellular assays, HEK-293 or CHO cells stably expressing human MC1R, MC3R, or MC5R are seeded in 96-well plates (40,000 cells/well) and cultured for 48 hours. Cells are loaded with a calcium-sensitive fluorescent dye (Fluo-4 AM, 2.5 microM) in HBSS buffer containing 20 mM HEPES and 2.5 mM probenecid for 60 minutes at 37degC. After washing, cells are pre-incubated with varying concentrations of MSG606 (0.1-1000 nM) for 10-15 minutes, followed by stimulation with an EC80 concentration of NDP-alpha-MSH (1-10 nM). Fluorescence intensity is measured using a fluorescence plate reader (excitation 485 nm, emission 525 nm). For cAMP accumulation assays, cells are treated with forskolin (1 microM) in the presence of MSG606, and cAMP levels are quantified by ELISA or HTRF. EC50 values for partial agonism at MC3R (59 nM) and MC5R (1300 nM) are determined from concentration-response curves.
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| Animal Protocol |
In vivo experiments with MSG606 typically use adult female CD-1 mice (20-30 g) to assess reversal of morphine-induced hyperalgesia. Morphine tolerance is induced by twice-daily subcutaneous administration of morphine (10 mg/kg) for 7 consecutive days. On day 8, a morphine challenge dose (5 mg/kg) is administered, followed by MSG606 (0.1-10 mg/kg) via intravenous, intraperitoneal, or subcutaneous injection. Mechanical hyperalgesia is assessed using von Frey filaments applied to the hind paw, with paw withdrawal threshold measured at 15, 30, 60, 120, and 180 minutes post-injection. The percent reversal of hyperalgesia is calculated compared to vehicle-treated controls. For neuroprotection studies, MSG606 is administered at 1-10 mg/kg in rodent models of neurodegeneration, with outcomes measured via behavioral testing and histological analysis of neuronal survival.
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| ADME/Pharmacokinetics |
As a peptide (molecular weight 1347.51 Da), MSG606 is not orally bioavailable and is typically administered via injection (IV, IP, or SC). The compound is soluble in water up to 1 mg/mL. Pharmacokinetic parameters are similar to other macrocyclic peptides: rapid distribution with a short plasma half-life (approximately 30-60 minutes) due to proteolytic degradation. Tissue distribution is primarily peripheral, with minimal blood-brain barrier penetration. Clearance occurs via renal filtration and proteolysis. No active metabolites have been characterized.
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| Toxicity/Toxicokinetics |
Limited toxicity data are available for MSG606. In preclinical studies at doses up to 10 mg/kg in mice, no significant adverse effects or mortality have been reported. Sex-specific differences in efficacy suggest potential hormonal modulation of responses. As with all research peptides, standard laboratory safety precautions should be followed. The compound has not undergone formal toxicological evaluation for clinical development. No genotoxicity or chronic toxicity studies have been publicly reported.
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| References | |
| Additional Infomation |
MSG606 is a gamma-MSH analogue with modifications including D-Phe at position 4 and D-Trp at position 6, with a carbasulfide bridge between the modified N-terminus and cysteine at position 7, and a C-terminal amide on glycine at position 11. The compound sequence is XGHFRWCDRFG. As a research tool, it has not entered clinical trials and is not approved by any regulatory agency for therapeutic use. CAS number: 1416983-77-1. Pure research chemical.
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| Molecular Formula |
C62H82N20O13S
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|---|---|
| Molecular Weight |
1347.50569009781
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| Exact Mass |
1346.609
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| CAS # |
1416983-77-1
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| Related CAS # |
MSG606 TFA
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| PubChem CID |
122177131
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| Appearance |
White to off-white solid powder
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| LogP |
-2.5
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| Hydrogen Bond Donor Count |
18
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| Hydrogen Bond Acceptor Count |
17
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| Rotatable Bond Count |
27
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| Heavy Atom Count |
96
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| Complexity |
2710
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| Defined Atom Stereocenter Count |
8
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| SMILES |
S1CCCC(NCC(N[C@@H](CC2=CN=CN2)C(N[C@@H](CC2C=CC=CC=2)C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@@H](CC(=O)O)C(N[C@H](C(N[C@H](C(NCC(N)=O)=O)CC2C=CC=CC=2)=O)CCC/N=C(\N)/N)=O)=O)C1)=O)CC1=CNC2C=CC=CC1=2)=O)CCC/N=C(\N)/N)=O)=O)=O)=O
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| InChi Key |
QJBNFEXQHBDMQM-VTWSTLNFSA-N
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| InChi Code |
InChI=1S/C62H82N20O13S/c63-49(83)31-73-53(88)43(24-35-12-3-1-4-13-35)78-54(89)41(18-9-21-69-61(64)65)77-59(94)47(28-52(86)87)81-60(95)48-33-96-23-11-20-50(84)72-32-51(85)75-46(27-38-30-68-34-74-38)58(93)79-44(25-36-14-5-2-6-15-36)56(91)76-42(19-10-22-70-62(66)67)55(90)80-45(57(92)82-48)26-37-29-71-40-17-8-7-16-39(37)40/h1-8,12-17,29-30,34,41-48,71H,9-11,18-28,31-33H2,(H2,63,83)(H,68,74)(H,72,84)(H,73,88)(H,75,85)(H,76,91)(H,77,94)(H,78,89)(H,79,93)(H,80,90)(H,81,95)(H,82,92)(H,86,87)(H4,64,65,69)(H4,66,67,70)/t41-,42-,43-,44-,45-,46-,47-,48-/m0/s1
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| Chemical Name |
(3S)-4-[[(2S)-1-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-1-oxo-3-phenylpropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-[[(3R,6S,9S,12S,15S)-12-benzyl-9-[3-(diaminomethylideneamino)propyl]-15-(1H-imidazol-5-ylmethyl)-6-(1H-indol-3-ylmethyl)-5,8,11,14,17,20-hexaoxo-1-thia-4,7,10,13,16,19-hexazacyclotricosane-3-carbonyl]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 (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) |
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 | 0.7421 mL | 3.7105 mL | 7.4211 mL | |
| 5 mM | 0.1484 mL | 0.7421 mL | 1.4842 mL | |
| 10 mM | 0.0742 mL | 0.3711 mL | 0.7421 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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