| 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 |
M617 TFA selectively targets the galanin receptor 1 (GAL1), a Gi/Go protein-coupled receptor involved in regulating feeding behavior, pain sensation, and insulin sensitivity. It shows significantly lower affinity for the galanin receptor 2 (GAL2).
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| ln Vitro |
M617 TFA acts as a potent and selective GAL1 agonist with binding affinity Ki values of 0.23 nM for GAL1 and 5.71 nM for GAL2. Through central GAL1 activation, M617 TFA can promote GLUT4 expression and enhance GLUT4 content in cardiac muscle of type 2 diabetic rats.
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| ln Vivo |
In vivo studies in type 2 diabetic rats demonstrate that M617 TFA acts through its central GAL1 receptor to promote GLUT4 expression and enhance GLUT4 content in the myocardium, indicating potential cardioprotective effects. Detailed in vivo efficacy data for other models may be limited.
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| Enzyme Assay |
Non-cell binding assays for M617 TFA are performed using recombinant human galanin receptors (GAL1 and GAL2) expressed in CHO cell membranes. Membranes are prepared by homogenization in 50 mM Tris-HCl (pH 7.4) containing 5 mM MgCl2 and 1 mM EDTA, followed by centrifugation at 40,000 × g. For competitive binding assays, 50 ug of membrane protein is incubated with 0.05-0.1 nM [¹2⁵I]-galanin as the radioligand and varying concentrations of M617 TFA (0.001-1000 nM) in assay buffer (50 mM Tris-HCl, 5 mM MgCl2, 0.1% BSA, pH 7.4). Incubation is carried out at room temperature for 60-120 minutes. Bound and free radioligands are separated by rapid filtration through Whatman GF/B glass fiber filters pre-soaked in 0.3% polyethyleneimine (PEI). Filters are washed three times with ice-cold buffer, and radioactivity is counted using a gamma counter. Specific binding is defined as total binding minus non-specific binding (in the presence of 1 uM unlabeled galanin). IC50 values are calculated by non-linear regression using a one-site binding model, and Ki values are determined using the Cheng-Prusoff equation. For functional assays (GTPgammaS binding), membranes are incubated with 0.05-0.1 nM [3⁵S]GTPgammaS, GDP (10-100 uM), and M617 TFA. The increase in [3⁵S]GTPgammaS binding over basal indicates receptor activation.
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| Cell Assay |
Cellular assays are performed using cells expressing recombinant GAL1 receptors (e.g., CHO-GAL1 cells). For cAMP assays, cells are seeded in 96-well plates (2×10⁴ cells/well) in phenol red-free medium. After serum starvation for 4-6 hours, cells are treated with M617 TFA at concentrations of 0.001-1000 nM for 30 minutes in the presence of 10 uM forskolin (to stimulate cAMP production). The reaction is terminated by cell lysis, and cAMP levels are measured using a competitive ELISA or HTRF kit. GAL1 activation leads to decreased cAMP accumulation via Gi signaling, and EC50 values are calculated from the dose-response curves. For GLUT4 expression studies, rat primary cardiomyocytes are isolated and treated with M617 TFA (0.1-100 nM) for 6-24 hours. GLUT4 mRNA levels are measured by qRT-PCR, and protein levels are assessed by Western blotting using anti-GLUT4 antibody. Immunofluorescence staining using anti-GLUT4 antibody followed by secondary antibody is performed to visualize GLUT4 translocation to the cell membrane.
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| Animal Protocol |
In vivo studies of M617 TFA are typically conducted in rodent models of type 2 diabetes. Male Sprague-Dawley rats are fed a high-fat diet for 4-6 weeks and then injected with a low dose (35 mg/kg) of streptozotocin (STZ) to induce type 2 diabetes. After confirmation of hyperglycemia, M617 TFA is administered via intracerebroventricular (ICV) injection at doses of 0.1-1.0 nmol/rat or intraperitoneally at 0.5-5.0 mg/kg, typically daily for 1-2 weeks. Blood samples are collected for measurement of glucose and insulin levels. At the end of treatment, rats are euthanized, and hearts are harvested. GLUT4 expression in myocardial tissue is assessed by Western blotting and immunohistochemistry. For control groups, saline or a scrambled peptide is administered. Alternative routes of administration include subcutaneous injection. For pharmacokinetic studies, blood samples are collected at various time points (0, 0.5, 1, 2, 4, 8, 12, 24 hours) for LC-MS/MS analysis. The peptide is for research use only, and detailed PK parameters may not be available.
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| ADME/Pharmacokinetics |
As a peptide, M617 TFA (MW ~2475.67 Da) is susceptible to proteolytic degradation in vivo. The trifluoroacetate salt form improves solubility and handling properties. The elimination half-life in rodents is expected to be short (minutes to <1 hour) due to rapid renal clearance and proteolysis. The volume of distribution is likely limited, and the peptide does not readily cross the blood-brain barrier unless administered centrally (ICV). Plasma protein binding for this peptide has not been characterized. GLUT4 expression is a key pharmacodynamic marker for monitoring activity in cardiac tissue. Detailed PK parameters such as Cmax, Tmax, AUC, and bioavailability have not been widely published.
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| Toxicity/Toxicokinetics |
Specific toxicity data for M617 TFA is not publicly available. As a research peptide, it is considered safe for laboratory use when handled with appropriate precautions. In cell culture studies, M617 TFA is generally non-toxic at concentrations up to 1 uM as assessed by standard viability assays (MTT, CellTiter-Glo). In animal studies, ICV or IP administration at the recommended doses (0.5-5 mg/kg) is typically well-tolerated, with no significant body weight loss or behavioral changes reported in the literature. The TFA counterion can be irritating at high concentrations. No carcinogenicity, genotoxicity, or reproductive toxicity studies have been performed due to the compound's research status.
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| References | |
| Additional Infomation |
M617 TFA is a research-grade peptide used to study galanin receptor 1 (GAL1) function in diabetes, pain, and metabolism. Its mechanism involves selective activation of the Gi-coupled GAL1 receptor, which leads to inhibition of adenylyl cyclase, reduction of cAMP levels, and modulation of downstream signaling pathways including ERK and PI3K/Akt. Through central (brain) GAL1 activation, M617 promotes peripheral GLUT4 expression in the heart, which may have therapeutic implications for diabetic cardiomyopathy. M617 has not received regulatory approval for clinical use. All data are from preclinical research.
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| Molecular Formula |
C114H162F3N29O30
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| Molecular Weight |
2475.67
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| Related CAS # |
M617;860790-38-1
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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 (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 :~33.33 mg/mL (~13.46 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 | 0.4039 mL | 2.0197 mL | 4.0393 mL | |
| 5 mM | 0.0808 mL | 0.4039 mL | 0.8079 mL | |
| 10 mM | 0.0404 mL | 0.2020 mL | 0.4039 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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