| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
RAGE antagonist peptide TFA targets the receptor for advanced glycation end‑products (RAGE), specifically binding to the extracellular V domain of the receptor. It prevents RAGE from binding to several of its most important ligands, including HMGB‑1, S100P, and S100A4. By blocking these interactions, the peptide inhibits downstream signaling pathways that lead to inflammation and cellular stress responses. This mechanism underlies its anti‑tumor and anti‑inflammatory activities.
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| ln Vitro |
In vitro, ligands' capacity to induce NFκB RAGE activation in cancer cells is diminished by the RAGE antagonist peptide TFA [1].
In vitro, RAGE antagonist peptide TFA blocks S100P, S100A4, and HMGB‑1 mediated RAGE activation. It inhibits RAGE‑mediated NF‑κB activity in human cells. In PDAC cells, RAGE‑mediated basal NF‑κB activity is inhibited in vitro by the peptide. These activities confirm its role as a RAGE antagonist and validate its use in studying RAGE‑mediated inflammatory and tumorigenic signaling. |
| ln Vivo |
In PDAC cells, RAGE-mediated basal NFκB activity is inhibited in vivo by RAGE antagonist peptide TFA (100 μg) [1]. Glioma growth can be inhibited and pancreatic tumor growth and metastasis can be decreased by RAGE antagonist peptide TFA [1]. The RAGE antagonist peptide TFA (RAP; 4 mg/kg; ip) decreased the release of Th2 cytokines and attenuated goblet cell metaplasia, airway inflammation, and airway responsiveness in mice with asthma. Additionally, RAGE antagonist peptide TFA can decrease β-catenin's total, cytoplasmic, and nuclear levels; increase β-catenin Ser33/37/Thr41 phosphorylation, which in turn causes ubiquitination; suppress β-catenin target gene expression; and prefer β-catenin to be retained at the cell membrane, which transforms β-catenin from an active mode of signaling to an adhesive function [2].
In vivo, RAGE antagonist peptide TFA (100 μg) inhibits RAGE‑mediated basal NF‑κB activity in PDAC cells. It reduces the growth and metastasis of pancreatic tumors and also inhibits glioma tumor growth. The peptide possesses anti‑tumor and anti‑inflammatory activities in various preclinical models. |
| Enzyme Assay |
Non‑cellular binding assays for RAGE antagonist peptide TFA involve measuring its ability to compete with natural ligands for binding to the RAGE V domain. These assays can be performed using ELISA‑based competition assays where the peptide is incubated with recombinant RAGE protein and labeled ligands such as S100P, S100A4, or HMGB‑1. The inhibition of ligand binding is quantified, and the peptide's potency is determined from dose‑response curves. Surface plasmon resonance (SPR) can also be employed to measure direct binding kinetics.
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| Cell Assay |
In vitro cellular assays for RAGE antagonist peptide TFA are performed using cells that express RAGE, such as PDAC cells or other cancer cell lines. Cells are treated with the peptide, and the inhibition of RAGE‑mediated NF‑κB activity is assessed using reporter assays or by measuring the expression of NF‑κB target genes. The peptide's effects on cell proliferation, migration, and invasion are also evaluated to confirm its anti‑tumor activity.
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| Animal Protocol |
Animal/Disease Models: Cancer cells expressing the NFκB-luc reporter implanted into immune-deficient mice[1].
Doses: 100 µg Route of Administration: Intratumoral delivery (or intraperitoneally (ip)). Experimental Results: Systemic administration caused a substantial reduction (p<0.05) in the NFκB signal 5 h after injection. In vivo animal experiments for RAGE antagonist peptide TFA are conducted in mouse models of cancer, such as pancreatic tumor xenografts and glioma models. The peptide is administered at a dose of 100 μg via appropriate routes (e.g., intraperitoneal injection), and endpoints include tumor growth inhibition, metastasis reduction, and assessment of NF‑κB activity in tumor tissues. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties for RAGE antagonist peptide TFA are not extensively detailed in available sources. The peptide has a molecular weight of approximately 1386.6 g/mol and a molecular formula of C59H102F3N13O19S. Its free base CAS number is 1092460‑91‑7. The sequence is Ac‑ELKVLMEKEL‑NH2 (Modifications: Glu‑1 = N‑terminal Ac, Leu‑10 = C‑terminal amide). The TFA salt form is used to enhance solubility and stability. It should be stored at -20°C.
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| Toxicity/Toxicokinetics |
Toxicological data for RAGE antagonist peptide TFA are not extensively detailed in available sources. As a peptide that inhibits RAGE signaling, it may modulate inflammatory responses and could have effects on normal tissue homeostasis. However, it is primarily used as a research tool in preclinical models and is not intended for human consumption. Comprehensive toxicological profiling would be required for any therapeutic development.
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| References | |
| Additional Infomation |
RAGE antagonist peptide TFA is a synthetic peptide that targets the RAGE receptor, blocking its interaction with key ligands including HMGB‑1, S100P, and S100A4. It has a molecular weight of approximately 1386.6 g/mol and a sequence of Ac‑ELKVLMEKEL‑NH2. It possesses anti‑tumor and anti‑inflammatory activities and is used as a research tool for studying RAGE‑mediated signaling. It is not approved for clinical use and is intended for research purposes only.
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| Molecular Formula |
C59H102F3N13O19S
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| Molecular Weight |
1386.58
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| Related CAS # |
RAGE antagonist peptide;1092460-91-7
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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) |
H2O :~25 mg/mL (~18.03 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 | 0.7212 mL | 3.6060 mL | 7.2120 mL | |
| 5 mM | 0.1442 mL | 0.7212 mL | 1.4424 mL | |
| 10 mM | 0.0721 mL | 0.3606 mL | 0.7212 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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