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| Targets |
This peptide is an ACE2-related peptide that spans a large portion of its N-terminal extracellular catalytic domain. Its primary utility is as a binding substrate or epitope for studying the interaction between ACE2 and other proteins, such as the SARS-CoV-2 spike protein or natural ligands like angiotensin II. While not an inhibitor itself, it can be used in competition assays to map binding sites. The parent protein, ACE2, is a zinc metalloprotease whose main physiological targets are Ang II and Ang I. By converting Ang II (a potent vasoconstrictor) into Ang 1-7 (a vasodilator), ACE2 plays a crucial counter-regulatory role within the RAS, protecting against hypertension, heart failure, and lung injury. This long peptide allows researchers to explore these binding and catalytic properties in a simplified, cell-free system.
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| ln Vitro |
No specific in vitro activity data for this exact peptide is available in the search results. However, the in vitro activity of the full-length ACE2 protein is well-established. Recombinant human ACE2 (rhACE2) is known to efficiently cleave the C-terminal phenylalanine residue from its substrate, Angiotensin II, to produce Angiotensin (1-7). The enzymatic activity of the ACE2 protein can be measured using fluorogenic peptide substrates, such as Mca-APK(Dnp)-OH, which fluoresces upon cleavage. This particular long peptide, representing the receptor binding domain (RBD), is more likely to be used in binding studies rather than enzymatic activity assays. It may interact with the natural ligands of ACE2, potentially blocking their binding to the active site.
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| ln Vivo |
No specific in vivo data for this peptide is available. The biological effects of the full-length ACE2 protein, however, are extensively characterized. Genetic deletion (knockout) of Ace2 in mice results in severe angiotensin II-dependent cardiac contractility defects, hypertension, and increased susceptibility to lung injury. Conversely, overexpression of ACE2 or administration of recombinant ACE2 is protective in animal models of hypertension, atherosclerosis, and acute respiratory distress syndrome (ARDS). The peptide may be used in vivo to block the interaction between viral proteins and ACE2, although its efficacy is not documented. Because it is a fragment, its in vivo activity is expected to be as a competitive binding agent rather than a catalytic enzyme.
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| Enzyme Assay |
A cell-free ELISA binding assay can be used to study the interaction of this ACE2 peptide with other proteins. A 96-well plate is coated with 1-5 microg/mL of the ACE2 peptide in coating buffer overnight at 4degC. The plate is then blocked with 3% BSA in PBS-T (0.05% Tween-20) for 1 hour at room temperature. Serially diluted recombinant SARS-CoV-2 spike protein (S1 subunit or RBD domain, 0.01-100 microg/mL) is added to the wells and incubated for 2 hours at 37degC. After washing, the plate is incubated with an HRP-conjugated antibody specific for the His-tag of the spike protein. The signal is developed with TMB substrate, stopped with H2SO4, and the absorbance is read at 450 nm. This protocol is used to map the interaction between the ACE2 receptor and the virus, and the long peptide can be used as a blocking reagent to test the specificity of the interaction.
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| Cell Assay |
A specific cell-based protocol for this exact peptide is not well-documented. However, researchers can perform a cell-based flow cytometry binding assay. ACE2-expressing cells, such as HEK293 cells transiently transfected with an ACE2 expression plasmid or naturally expressing A549 human lung epithelial cells, are detached and resuspended in FACS buffer (PBS + 1% BSA). The cells are then incubated with varying concentrations of the ACE2-related peptide (e.g., 0.1-100 microM) on ice for 30 minutes. After washing, the bound peptide can be detected using a primary antibody specific for the peptide's sequence (if available) followed by a fluorescently-labeled secondary antibody. Alternatively, the biotinylated form of the peptide can be used, followed by detection with Streptavidin-PE. The cells are then analyzed by flow cytometry. A shift in mean fluorescence intensity (MFI) indicates binding. This experiment can be used to determine the Kd of the peptide for the ACE2 receptor on the cell surface.
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| Animal Protocol |
An in vivo protocol for this peptide might involve a xenograft mouse model for imaging studies. For an imaging experiment, the peptide could be conjugated to a near-infrared (NIR) dye (e.g., Cy5.5 or IRDye 800CW) to create an optical tracer. To study ACE2 expression in tumors or inflammation, female BALB/c nude mice (6-8 weeks) are injected subcutaneously with 5×10⁶ ACE2-positive tumor cells (e.g., A549 lung cancer cells). When the tumor volume reaches 200-300 mm3, the labeled peptide (5-10 mg/kg) is administered intravenously via the tail vein. In vivo imaging is performed using an IVIS Spectrum or similar imaging system at various time points (0, 1, 2, 4, 6, 8, 24 hours post-injection). The region of interest (ROI) is measured to quantify the fluorescence intensity in the tumor, and blocking studies with an excess of unlabeled peptide (50-100 mg/kg) are used to confirm specificity. Ex vivo biodistribution is performed at the end of the experiment.
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| ADME/Pharmacokinetics |
This product is a lyophilized white to off-white solid powder with high purity (≥98%). It should be stored in a sealed container at -20degC, protected from moisture, where it is stable for up to 3 years. For long-term storage of solutions, it is recommended to store at -80degC for up to 6 months. It is soluble in DMSO at ~33.33 mg/mL (~6.89 mM). For in vivo administration, a formulation protocol is available: the peptide can be dissolved to ≥ 2.5 mg/mL (0.52 mM) in a solution of 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline, creating a clear solution suitable for injection. Because of its high molecular weight (4835.47 g/mol), it will have a relatively long half-life in circulation but will primarily be cleared by the reticuloendothelial system.
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| Toxicity/Toxicokinetics |
This product is for research use only and is not intended for diagnostic or therapeutic use in humans. As a research-grade peptide with a TFA salt, no specific toxicity data is available. The TFA counterion can be problematic in cell culture if the concentration exceeds 0.1%, but for most in vivo and in vitro applications, this is not an issue at working dilutions. Standard laboratory safety practices, including the use of personal protective equipment (PPE) such as gloves and safety glasses, should be followed. The primary caution is that, due to its long sequence, handling and storage must be carefully managed to avoid degradation and aggregation of the peptide.
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| Additional Infomation |
This long-chain peptide (the sequence is 36 amino acids long) is a research tool designed for studying protein-protein interactions involving ACE2. The human ACE2 protein is a critical component of the Renin-Angiotensin-Aldosterone System (RAAS), counterbalancing ACE by degrading Angiotensin II, a potent vasoconstrictor, into Angiotensin 1-7, a vasodilator. This peptide is derived from the region that interacts with viral spike proteins, making it highly relevant for research related to infectious diseases. The TFA salt form is a common synthetic counterion used to improve the physicochemical properties of peptides for research applications. The peptide's high molecular weight (approx. 4835 Da) is typical of large synthetic fragments used in protein interaction studies.
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| Molecular Formula |
C213H342N58O66S2
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| Molecular Weight |
4835.47
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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 :~33.33 mg/mL (~6.89 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (0.52 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 (0.52 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.2068 mL | 1.0340 mL | 2.0681 mL | |
| 5 mM | 0.0414 mL | 0.2068 mL | 0.4136 mL | |
| 10 mM | 0.0207 mL | 0.1034 mL | 0.2068 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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