| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
MC3R
PG106 TFA targets the human melanocortin 3 (hMC3) receptor with high selectivity. It is a potent antagonist with an IC50 value of 210 nM for the hMC3 receptor. The compound exhibits negligible activity at the hMC4 receptor (EC50 = 9900 nM) and the hMC5 receptor, demonstrating its selectivity for the MC3 receptor. By blocking MC3 receptor signaling, it modulates melanocortin‑mediated pathways involved in appetite regulation, energy homeostasis, and central control of body weight. |
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| ln Vitro |
In vitro, PG106 TFA is a potent and selective hMC3 receptor antagonist with an IC50 of 210 nM. It shows no significant activity at hMC4 receptors (EC50 = 9900 nM) and hMC5 receptors, confirming its selectivity for MC3. This selectivity profile makes it a valuable tool for dissecting MC3‑ versus MC4‑mediated effects in melanocortin signaling studies.
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| ln Vivo |
Specific in vivo activity data for PG106 TFA are not extensively detailed in available sources. As a selective hMC3 receptor antagonist, it may have potential for in vivo studies in neuroendocrine and metabolic research. The TFA salt supports consistent parenteral dosing preparation.
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| Enzyme Assay |
Non‑cellular receptor binding assays for PG106 TFA involve measuring its binding affinity to melanocortin receptors using radioligand displacement techniques. The compound is incubated with membranes expressing hMC3, hMC4, or hMC5 receptors and a labeled ligand. The displacement of the radioligand is quantified, and IC50 or EC50 values are determined from competitive binding curves.
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| Cell Assay |
In vitro cellular assays for PG106 TFA are performed using cells expressing melanocortin receptors to assess receptor antagonism. Cells expressing hMC3, hMC4, or hMC5 receptors are treated with the compound, and the inhibition of receptor‑mediated signaling (e.g., cAMP production) is measured. IC50 and EC50 values are determined from dose‑response curves.
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| Animal Protocol |
In vivo animal experiments for PG106 TFA would typically be conducted in rodent models to study the role of MC3 receptors in appetite regulation, energy homeostasis, and body weight control. The compound would be administered via intraperitoneal or intracerebroventricular injection, and endpoints would include food intake, body weight, and metabolic parameters.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties for PG106 TFA are not extensively detailed in available sources. The peptide has a molecular weight of 1122.20 and a molecular formula of C53H70F3N13O11. The sequence is Ac‑{Nle}‑D‑{Bal}‑{D‑Nal}‑RWK‑NH2 with a lactam bridge between Asp2 and Lys7. It is soluble in DMSO (~25 mg/mL) and can be formulated for in vivo administration. It should be stored in a sealed container, away from moisture, at -80°C for up to 2 years.
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| Toxicity/Toxicokinetics |
Toxicological data for PG106 TFA are not extensively detailed in available sources. As a research peptide, its safety profile has not been extensively characterized. It is intended for research use only and not for human consumption. Comprehensive toxicological studies would be required for any therapeutic development.
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| References | |
| Additional Infomation |
PG106 TFA is a potent and selective hMC3 receptor antagonist with an IC50 of 210 nM. It shows negligible activity at hMC4 receptors (EC50 = 9900 nM) and hMC5 receptors. It is a synthetic cyclic peptide derived from the α‑MSH scaffold and is used as a research tool for studying melanocortin receptor signaling. It is not approved for clinical use.
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| Molecular Formula |
C53H70F3N13O11
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|---|---|
| Molecular Weight |
1122.20
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| Related CAS # |
PG106;944111-22-2
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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) |
DMSO :~25 mg/mL (~22.28 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.23 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (2.23 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (2.23 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.8911 mL | 4.4555 mL | 8.9111 mL | |
| 5 mM | 0.1782 mL | 0.8911 mL | 1.7822 mL | |
| 10 mM | 0.0891 mL | 0.4456 mL | 0.8911 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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