| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
Purity: =98.53%
| Targets |
RAGE antagonist peptide targets the Receptor for Advanced Glycation End Products (RAGE). It prevents RAGE from binding with several of its most important ligands, including HMGB-1, S100P, and S100A4. By blocking these interactions, the peptide inhibits RAGE-mediated signaling pathways, including NFκB activation. RAGE is involved in inflammation, cancer progression, and diabetic complications, making it a therapeutic target for various diseases.
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| ln Vitro |
The ability of ligands to promote RAGE activation of NFκB in cancer cells in vitro is reduced by RAGE antagonist peptide (RAP)[1].
In vitro, RAGE antagonist peptide (RAP) reduces the ability of the ligands to stimulate RAGE activation of NFκB in cancer cells. The peptide blocks S100P, S100A4, and HMGB-1 mediated RAGE activation. This inhibition of RAGE signaling results in reduced inflammatory and tumor-promoting effects. Standard in vitro assays include NFκB reporter assays, ELISA-based binding studies to measure ligand displacement, and assessment of downstream signaling markers such as cytokine production and cell proliferation. |
| ln Vivo |
In vivo, PDAC cells' RAGE-mediated Basal NFκB Activity is inhibited by RAGE antagonist peptide (RAP, 100 µg)[1]. RAGE antagonist peptide (RAP) inhibits the growth of glioma tumors and decreases the growth and spread of pancreatic cancers[1]. RAGE antagonist peptide (RAP; 4 mg/kg; ip) blunts goblet cell metaplasia, airway inflammation, and airway responsiveness in asthmatic mice while also reducing Th2 cytokine secretion. In addition, RAGE antagonist peptide decreases β-catenin levels in the cytoplasm, nucleus, and total body. It also increases β-catenin phosphorylation at Ser33/37/Thr41, which results in ubiquitination, downregulates the expression of genes targeted by β-catenin, and keeps β-catenin at the cytomembrane, converting it from an active signaling pattern to an adhesive function[2].
In vivo, RAGE antagonist peptide inhibits growth and metastasis of rat glioma tumors. The peptide possesses anti-tumor and anti-inflammatory activities. It has been shown to block RAGE-mediated signaling in various disease models. The compound's ability to inhibit tumor growth and metastasis suggests potential therapeutic applications in oncology. However, comprehensive in vivo efficacy data from published literature are limited. The compound is used in preclinical research to study RAGE-related pathologies. |
| Enzyme Assay |
For non-cell-based receptor binding assays, RAGE antagonist peptide can be evaluated using purified RAGE protein. Binding affinity is assessed using surface plasmon resonance (SPR) or ELISA-based binding assays. Purified RAGE is immobilized on sensor chips or ELISA plates, and increasing concentrations of the peptide are applied. Competitive binding experiments are performed using labeled ligands (HMGB-1, S100P, or S100A4) to assess the peptide's ability to displace ligand binding. Binding kinetics and dissociation constants are calculated from the binding data.
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| Cell Assay |
For in vitro cellular assays, cancer cells or immune cells expressing RAGE are cultured in appropriate media. Cells are treated with RAGE ligands (HMGB-1, S100P, or S100A4) in the presence or absence of RAGE antagonist peptide. NFκB activation is measured using luciferase reporter assays or by assessing nuclear translocation of NFκB using immunofluorescence. Cytokine production (e.g., TNFα, IL-6) is measured using ELISA. Cell proliferation and migration assays are performed to assess the peptide's effects on tumor cell behavior.
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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). Experimental Results: Systemic administration caused a substantial reduction ( p<0.05) in the NFκB signal 5 h after injection. For in vivo animal studies, RAGE antagonist peptide is typically administered to rodents via intraperitoneal injection. In glioma tumor models, tumor growth and metastasis are monitored following peptide treatment. In inflammation models, inflammatory markers and tissue damage are assessed. In diabetic complications models, renal function and neuropathy are evaluated. Dosing regimens vary depending on the specific model. Blood and tissue samples may be collected for pharmacokinetic and pharmacodynamic analysis. |
| ADME/Pharmacokinetics |
RAGE antagonist peptide has a molecular weight of 1272.56 and a molecular formula of C57H101N13O17S. It is a peptide with the sequence Ac-ELKVLMEKEL-NH2. The peptide has both N-terminal and C-terminal modifications for improved stability. It is supplied as a white powder with a purity of ≥98.0% by HPLC. The compound should be stored under recommended conditions. It is for research use only and not for human consumption.
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| Toxicity/Toxicokinetics |
The toxicity profile of RAGE antagonist peptide has not been extensively reported. As a peptide antagonist of RAGE, it is expected to have a favorable safety profile due to its specificity for the RAGE receptor. The compound is for research use only and not for human consumption. Standard toxicological evaluation would include acute and repeated-dose toxicity studies, as well as assessment of effects on the immune system and tumor growth. Potential adverse effects may include immunosuppression due to inhibition of RAGE-mediated inflammatory responses.
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| References | |
| Additional Infomation |
RAGE antagonist peptide (RAP) is an advanced glycation end products (RAGE) antagonist that prevents RAGE from binding with several of its most important ligands, including HMGB-1, S100P, and S100A4. It possesses anti-tumor and anti-inflammatory activities. The peptide inhibits growth and metastasis of rat glioma tumors. It reduces the ability of the ligands to stimulate RAGE activation of NFκB in cancer cells in vitro. It is available for research purposes only.
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| Molecular Formula |
C57H101N13O17S
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|---|---|
| Molecular Weight |
1272.56
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| Exact Mass |
1271.715
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| CAS # |
1092460-91-7
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| Related CAS # |
RAGE antagonist peptide TFA
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| PubChem CID |
127021052
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| Appearance |
White to off-white solid powder
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| LogP |
-4.4
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| Hydrogen Bond Donor Count |
16
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| Hydrogen Bond Acceptor Count |
20
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| Rotatable Bond Count |
47
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| Heavy Atom Count |
88
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| Complexity |
2330
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| Defined Atom Stereocenter Count |
10
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| SMILES |
S(C)CC[C@@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N)=O)CC(C)C)=O)CCC(=O)O)=O)CCCCN)=O)CCC(=O)O)=O)NC([C@H](CC(C)C)NC([C@H](C(C)C)NC([C@H](CCCCN)NC([C@H](CC(C)C)NC([C@H](CCC(=O)O)NC(C)=O)=O)=O)=O)=O)=O
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| InChi Key |
UPCWJIBXKJZZLN-RBQIHDOFSA-N
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| InChi Code |
InChI=1S/C57H101N13O17S/c1-30(2)27-41(48(60)78)67-52(82)39(19-22-46(76)77)64-49(79)35(15-11-13-24-58)62-51(81)38(18-21-45(74)75)65-53(83)40(23-26-88-10)66-56(86)43(29-32(5)6)69-57(87)47(33(7)8)70-54(84)36(16-12-14-25-59)63-55(85)42(28-31(3)4)68-50(80)37(61-34(9)71)17-20-44(72)73/h30-33,35-43,47H,11-29,58-59H2,1-10H3,(H2,60,78)(H,61,71)(H,62,81)(H,63,85)(H,64,79)(H,65,83)(H,66,86)(H,67,82)(H,68,80)(H,69,87)(H,70,84)(H,72,73)(H,74,75)(H,76,77)/t35-,36-,37-,38-,39-,40-,41-,42-,43-,47-/m0/s1
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| Chemical Name |
(4S)-4-acetamido-5-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-oxopentanoic acid
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 0.7858 mL | 3.9291 mL | 7.8582 mL | |
| 5 mM | 0.1572 mL | 0.7858 mL | 1.5716 mL | |
| 10 mM | 0.0786 mL | 0.3929 mL | 0.7858 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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