| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 100mg |
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| Other Sizes |
| Targets |
MC4R
HS014 TFA targets the melanocortin-4 (MC4) receptor with high selectivity. It exhibits Ki values of 3.16 nM for human MC4, 108 nM for MC1, 54.4 nM for MC3, and 694 nM for MC5 receptors. This selectivity profile makes it a valuable tool for studying MC4 receptor function. |
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| ln Vitro |
In vitro, HS014 TFA acts as a potent and selective MC4 receptor antagonist. Its binding affinity for MC4 (Ki = 3.16 nM) is significantly higher than for other melanocortin receptor subtypes, confirming its selectivity.
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| ln Vivo |
When HS014 TFA is pretreated, it improves metabolic rate and prevents the effects of IL-1beta on food intake, respiratory exchange ratio (RER), and hypoactivity at later times (after 8 hours post-injection)[2].
In vivo, HS014 TFA increases food intake in free-feeding rats, demonstrating its role in blocking MC4 receptor-mediated satiety signaling. Pretreatment with HS014 TFA blocks IL-1beta-induced effects on food intake, respiratory exchange rate (RER), hypoactivity, and increased metabolic rate at later time points (8 hours post-injection). |
| Enzyme Assay |
Non-cellular receptor binding assays for HS014 TFA involve measuring its binding affinity to melanocortin receptors using radioligand binding techniques. The compound is incubated with membranes expressing MC4, MC1, MC3, or MC5 receptors and a labeled ligand, and the displacement is quantified to determine Ki values.
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| Cell Assay |
In vitro cellular assays for HS014 TFA are performed using cells expressing melanocortin receptors to assess receptor antagonism. The compound's ability to inhibit MC4 receptor-mediated signaling, such as cAMP production, is measured to confirm its antagonistic activity.
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| Animal Protocol |
In vivo animal experiments for HS014 TFA are conducted in rat models to study feeding behavior and energy metabolism. The compound is administered via appropriate routes, and endpoints include measurement of food intake, respiratory exchange rate, and locomotor activity.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties for HS014 TFA are not detailed in available sources. The compound has a molecular weight of 1677.78 and a molecular formula of C73H95F3N20O19S2. It is a solid, white to off-white powder with a sequence of Ac-Cys-Glu-His-{D-2Nal}-Arg-Trp-Gly-Cys-Pro-Pro-Lys-Asp-NH2 (disulfide bridge: Cys1-Cys8).
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| Toxicity/Toxicokinetics |
Toxicological data for HS014 TFA are not provided 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.
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| References | |
| Additional Infomation |
HS014 TFA is a potent and selective MC4 receptor antagonist with Kis of 3.16, 108, 54.4 and 694 nM for human MC4, MC1, MC3 and MC5 receptors respectively. It is used as a research tool for studying melanocortin receptor biology. No clinical trial or regulatory approval information is available.
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| Molecular Formula |
C73H95F3N20O19S2
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|---|---|
| Molecular Weight |
1677.78
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| Related CAS # |
HS014;207678-81-7
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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 :~100 mg/mL (~59.60 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (1.49 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 (1.49 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 (1.49 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 | 0.5960 mL | 2.9801 mL | 5.9603 mL | |
| 5 mM | 0.1192 mL | 0.5960 mL | 1.1921 mL | |
| 10 mM | 0.0596 mL | 0.2980 mL | 0.5960 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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