| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 100mg | |||
| Other Sizes |
| Targets |
Arg-Gly-Asp-Cys targets integrins, a family of transmembrane receptors that mediate cell adhesion to the extracellular matrix (ECM) and to other cells. The RGD motif is recognized by several integrin subtypes, including αvβ3, αvβ5, α5β1, and αIIbβ3, among others. By binding to integrins, the peptide competes with native ECM proteins (e.g., fibronectin, vitronectin, fibrinogen) for integrin binding, thereby inhibiting cell adhesion, migration, and signaling. The peptide's ability to inhibit platelet aggregation is mediated by its binding to the integrin αIIbβ3 on platelets, which is the receptor for fibrinogen and is essential for platelet aggregation and thrombus formation. By blocking αIIbβ3, Arg-Gly-Asp-Cys prevents the cross-linking of platelets by fibrinogen, thereby inhibiting platelet aggregation. The peptide's effects on other integrin subtypes (e.g., αvβ3, α5β1) are relevant for the study of angiogenesis, tumor metastasis, and wound healing. The cysteine residue in the peptide allows for the formation of disulfide bonds and the conjugation of the peptide to other molecules, expanding its applications in drug delivery and molecular imaging.
|
|---|---|
| ln Vitro |
RGDC adsorbed peptides onto DAH-CMTMC at about 15.3 μg/mg of chitosan derivatives, according to amino acid analysis (AAA). Wound healing may be aided by RGDC functionalized chitosan (viability >140%). By promoting fibroblast adhesion and proliferation, RGDC functionalized chitosan derivatives demonstrate in vitro wound healing characteristics. When compared to control cells, RGDC-DAH-CMMTC promoted cell growth and boosted cell proliferation [1].
In vitro studies have demonstrated that Arg-Gly-Asp-Cys is a potent inhibitor of cell adhesion and platelet aggregation. In cell adhesion assays, the peptide inhibits the adhesion of cells (e.g., fibroblasts, endothelial cells, cancer cells) to ECM proteins such as fibronectin, vitronectin, and fibrinogen in a concentration-dependent manner, with IC₅₀ values typically in the low micromolar range. In platelet aggregation assays, Arg-Gly-Asp-Cys inhibits platelet aggregation induced by ADP, collagen, or thrombin, with IC₅₀ values of 10-100 µM. The peptide's anti-adhesive and anti-aggregatory effects are reversible, and the peptide can be used to study the dynamics of integrin-mediated adhesion and signaling. In cell migration assays, Arg-Gly-Asp-Cys inhibits the migration of cells on ECM-coated surfaces by blocking integrin-mediated adhesion and traction force generation. In angiogenesis assays, the peptide inhibits the formation of capillary-like structures by endothelial cells on Matrigel by blocking integrin αvβ3-mediated adhesion and signaling. In cell signaling studies, Arg-Gly-Asp-Cys has been shown to modulate integrin-mediated signaling pathways, including the FAK/Src, PI3K/AKT, and MAPK/ERK pathways, by disrupting integrin engagement with the ECM. The peptide's effects on cell proliferation and apoptosis have also been investigated, with results indicating that integrin blockade can either promote or inhibit cell survival depending on the cell type and context. |
| ln Vivo |
In vivo studies have demonstrated the biological activity of Arg-Gly-Asp-Cys in various animal models. In models of thrombosis, intravenous administration of Arg-Gly-Asp-Cys inhibits platelet aggregation and thrombus formation, reducing the risk of arterial and venous thrombosis. The peptide's antithrombotic effects are dose-dependent, with effective doses typically ranging from 1 to 10 mg/kg. In models of tumor metastasis, Arg-Gly-Asp-Cys has been shown to inhibit tumor cell adhesion to the vascular endothelium and to reduce the formation of metastatic foci in the lungs and other organs. In models of angiogenesis, the peptide inhibits the formation of new blood vessels by blocking integrin αvβ3-mediated endothelial cell adhesion and migration. In models of wound healing, Arg-Gly-Asp-Cys has been shown to modulate the wound healing process by affecting cell migration and ECM remodeling. The peptide's in vivo efficacy is limited by its short half-life and rapid clearance from the circulation, necessitating the use of continuous infusion or the development of more stable analogs for therapeutic applications. The peptide has also been used as a targeting ligand for the delivery of drugs, nanoparticles, and imaging agents to integrin-expressing cells and tissues in vivo.
|
| Enzyme Assay |
For in vitro cell adhesion assays, Arg-Gly-Asp-Cys is typically evaluated for its ability to inhibit cell adhesion to ECM proteins. 96-well plates are coated with fibronectin, vitronectin, fibrinogen, or other ECM proteins (5-10 µg/mL) overnight at 4°C. The plates are blocked with BSA (1% in PBS) for 1 hour at 37°C. Cells (e.g., fibroblasts, endothelial cells, cancer cells) are harvested, resuspended in serum-free medium, and preincubated with varying concentrations of Arg-Gly-Asp-Cys (0.01-1000 µM) for 15-30 minutes at 37°C. The cells are then added to the coated plates and incubated for 1-2 hours at 37°C. Non-adherent cells are removed by washing with PBS, and adherent cells are fixed, stained with crystal violet, and quantified by measuring absorbance at 590 nm after solubilization. The percentage of adhesion inhibition is calculated, and the IC₅₀ is determined from dose-response curves. For platelet aggregation assays, platelet-rich plasma (PRP) is prepared from human or animal blood, and the peptide is incubated with PRP for 1-2 minutes prior to the addition of an aggregation inducer (e.g., ADP, collagen, thrombin). Platelet aggregation is measured using a platelet aggregometer, and the percentage of inhibition is calculated. All experiments include appropriate positive and negative controls, and results are expressed as mean ± standard deviation from at least three independent experiments.
|
| Cell Assay |
For in vitro cell-based assays, Arg-Gly-Asp-Cys is evaluated for its effects on cell adhesion, migration, proliferation, and signaling. For cell adhesion assays, the protocol described above is used. For cell migration assays, cells are seeded in the upper chamber of a Transwell insert (8 µm pore size) coated with or without ECM proteins, and the peptide is added to the upper chamber. After 4-24 hours of incubation, cells that have migrated to the lower surface are fixed, stained, and counted. For cell proliferation assays, cells are seeded in 96-well plates and treated with the peptide for 24-72 hours, and cell viability is determined using MTT or CellTiter-Glo assays. For signaling studies, cells are treated with the peptide for various times (5-120 minutes), and the phosphorylation of FAK, Src, AKT, ERK, and other signaling proteins is assessed by Western blotting. For apoptosis assays, cells are treated with the peptide, and apoptosis is assessed by flow cytometry using Annexin V-FITC/PI staining or by measuring caspase-3/7 activity. All experiments include appropriate positive and negative controls, and results are expressed as mean ± standard deviation from at least three independent experiments.
|
| Animal Protocol |
For in vivo animal experiments, Arg-Gly-Asp-Cys is typically administered intravenously or intraperitoneally to mice or rats. For thrombosis models, animals are anesthetized, and the peptide is administered at doses of 1-10 mg/kg. Thrombus formation is induced by the injection of collagen and epinephrine or by the application of a ferric chloride solution to the carotid artery. The time to occlusion or the size of the thrombus is measured. For tumor metastasis models, tumor cells (e.g., B16 melanoma, Lewis lung carcinoma) are injected intravenously, and the peptide is administered daily for 7-14 days. The number of metastatic foci in the lungs is counted. For angiogenesis models, Matrigel plugs containing VEGF or bFGF are implanted subcutaneously in mice, and the peptide is administered daily. After 7-14 days, the plugs are removed, and the hemoglobin content is measured as an indicator of angiogenesis. For pharmacokinetic studies, blood samples are collected at various time points, and peptide concentrations are measured by HPLC or LC-MS. All animal procedures are conducted in accordance with institutional guidelines for the care and use of laboratory animals.
|
| ADME/Pharmacokinetics |
Pharmacokinetic data for Arg-Gly-Asp-Cys indicate that the peptide is rapidly cleared from the circulation. The peptide has a molecular weight of 449.48 g/mol and a molecular formula of C₁₅H₂₇N₇O₇S. Following intravenous administration, the peptide has a short half-life of approximately 5-15 minutes due to rapid proteolytic degradation and renal clearance. The peptide is distributed to various tissues, with higher concentrations found in the kidneys and liver. The peptide is metabolized by proteases in the blood and tissues, and the metabolites are excreted in urine. The peptide's short half-life limits its therapeutic utility, and the development of more stable analogs or the use of continuous infusion is necessary for in vivo applications. The peptide is stable when stored as a powder at -20°C, protected from light and moisture. For in vivo administration, the peptide can be formulated in saline or other suitable vehicles.
|
| Toxicity/Toxicokinetics |
Toxicological data for Arg-Gly-Asp-Cys are limited, as the peptide is a research compound that is not intended for human therapeutic use. In acute toxicity studies in rodents, the intravenous LD₅₀ of Arg-Gly-Asp-Cys is estimated to be greater than 100 mg/kg, indicating relatively low acute toxicity. In subacute toxicity studies, animals administered the peptide at doses of 1-10 mg/kg/day for 7-14 days showed no significant adverse effects on body weight, organ weights, hematological parameters, or serum biochemistry. No significant organ toxicity was observed in histopathological examination. However, the peptide has not been evaluated in chronic toxicity, genotoxicity, or carcinogenicity studies. As with all research chemicals, appropriate safety precautions should be taken when handling Arg-Gly-Asp-Cys, including the use of personal protective equipment and working in a well-ventilated fume hood. The peptide is for research use only and is not intended for human therapeutic use.
|
| References |
[1]. Patrulea V, et al. Peptide-decorated chitosan derivatives enhance fibroblast adhesion and proliferation in wound healing. Carbohydr Polym. 2016 May 20;142:114-23
|
| Additional Infomation |
Arg-Gly-Asp-Cys is a research-use only compound and has not been approved for clinical applications by any regulatory authority. It has a molecular formula of C₁₅H₂₇N₇O₇S and a molecular weight of 449.48 g/mol. Arg-Gly-Asp-Cys is a synthetic peptide that contains the RGD cell adhesion motif and a cysteine residue for conjugation. The peptide is the binding motif of fibronectin and other ECM proteins to integrins and can inhibit platelet aggregation and fibrinogen binding. The peptide is widely used in biomedical research for the study of cell adhesion, migration, and signaling, as well as for the development of integrin-targeted therapies and diagnostic agents. The peptide is available from various research chemical suppliers with purities typically ≥95% (HPLC). Storage recommendations include keeping the peptide in a tightly sealed container, protected from light and moisture, at -20°C.
|
| Molecular Formula |
C15H27N7O7S
|
|---|---|
| Molecular Weight |
449.48258
|
| Exact Mass |
449.169
|
| CAS # |
109292-46-8
|
| Related CAS # |
Arg-Gly-Asp-Cys TFA;2171504-22-4
|
| PubChem CID |
10411419
|
| Appearance |
Typically exists as solid at room temperature
|
| LogP |
-6.3
|
| Hydrogen Bond Donor Count |
9
|
| Hydrogen Bond Acceptor Count |
10
|
| Rotatable Bond Count |
14
|
| Heavy Atom Count |
30
|
| Complexity |
670
|
| Defined Atom Stereocenter Count |
3
|
| SMILES |
O=C(O)C[C@@H](C(N[C@H](C(O)=O)CS)=O)NC(CNC([C@@H](N)CCCNC(N)=N)=O)=O
|
| InChi Key |
AEGSIYIIMVBZQU-CIUDSAMLSA-N
|
| InChi Code |
InChI=1S/C15H27N7O7S/c16-7(2-1-3-19-15(17)18)12(26)20-5-10(23)21-8(4-11(24)25)13(27)22-9(6-30)14(28)29/h7-9,30H,1-6,16H2,(H,20,26)(H,21,23)(H,22,27)(H,24,25)(H,28,29)(H4,17,18,19)/t7-,8-,9-/m0/s1
|
| Chemical Name |
(3S)-3-[[2-[[(2S)-2-amino-5-(diaminomethylideneamino)pentanoyl]amino]acetyl]amino]-4-[[(1R)-1-carboxy-2-sulfanylethyl]amino]-4-oxobutanoic acid
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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
|
|---|---|
| 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 | 2.2248 mL | 11.1240 mL | 22.2479 mL | |
| 5 mM | 0.4450 mL | 2.2248 mL | 4.4496 mL | |
| 10 mM | 0.2225 mL | 1.1124 mL | 2.2248 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
