| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Integrins, specifically alphavbeta3, alphavbeta5, alphaIIbbeta3, and alpha5beta1 integrins. The RGD tripeptide sequence is a core recognition motif for many adhesion proteins like fibronectin, vitronectin, and fibrinogen. The RGDC peptide acts as a competitive inhibitor, binding to the integrin's binding pocket and preventing the docking of larger, natural ligands (e.g., fibrinogen). It also has an additional cysteine residue for site-specific conjugation.
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| ln Vitro |
In comparison to the control cells (viability >140%), Arg-Gly-Asp-Cys-functionalized chitosan (0.25-1 mg/mL; 2-7 days) promotes cell development and an increase in cellular proliferation[1]. -Asp-Cys-functionalized chitosan derivatives improve fibroblast adhesion and proliferation, which exhibits in vitro wound healing properties[1].
In vitro, RGDC inhibits the binding of fibrinogen to ADP-stimulated platelets with an IC50 of 35 uM and to endothelial cells with an IC50 of 320 uM. It also effectively inhibits blood platelet aggregation. As a soluble competitor, it can detach cells from their extracellular matrix (ECM) and inhibit cell adhesion. It has been conjugated to surfaces to promote cell adhesion, which improves gene transfection efficiency and bone growth on implants. |
| ln Vivo |
When coated onto titanium implants, RGDC has been shown to increase bone formation in rat femurs. When conjugated to polyethylenimine, it improves gene transfection efficiency by targeting the polymer-DNA complex to integrins on the cell surface. The cyclic form of this peptide (Ac-Pen-Arg-Gly-Asp-Cys-OH, cyclic RGDC) is a more potent inhibitor of platelet aggregation, with an IC50 of 0.55 microM, showing the importance of structural constraints.
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| Enzyme Assay |
The standard assay for RGDC is a competitive binding assay using purified integrin and a labeled ligand. For example, the alphaIIbbeta3 integrin (the platelet fibrinogen receptor) can be immobilized on a 96-well plate. A fixed concentration of biotinylated fibrinogen is added, along with varying concentrations of the test peptide. After incubation, the amount of bound fibrinogen is measured with HRP-labeled streptavidin. The half-maximal inhibitory concentration (IC50) is determined from the competition curve.
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| Cell Assay |
A functional cellular assay for RGDC is a cell adhesion assay. 96-well plates are coated with an adhesion protein (e.g., fibronectin or fibrinogen). Cells (e.g., platelets or endothelial cells) are pre-incubated with varying concentrations of the RGDC peptide and then added to the coated wells. After allowing time for adhesion, non-adherent cells are washed away, and the number of adherent cells is quantified using a fluorescence stain (e.g., Calcein-AM) or a colorimetric method (e.g., crystal violet). A reduction in adhesion signifies inhibition of integrin binding.
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| Animal Protocol |
The in vivo efficacy of RGDC has been assessed in a rat model of bone growth. In this model, commercially pure titanium rods were coated with RGDC via a chemical linker. These rods were then implanted into the femurs of rats. After several weeks, the amount of new bone formation around the implant was measured by histomorphometry. The RGDC-coated implants resulted in significantly increased bone apposition compared to uncoated controls, demonstrating its ability to promote osteointegration.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of RGDC are typical of a small, unmodified peptide. It has a poor oral bioavailability and a very short plasma half-life (on the order of minutes) due to rapid degradation by ubiquitous serum and tissue proteases. For in vivo studies, it is typically used by local administration (e.g., coated on an implant, or injected directly into a tissue) to achieve a high local concentration and minimize systemic degradation.
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| Toxicity/Toxicokinetics |
RGDC is considered a low-toxicity research tool. Short peptides like RGDC are generally biocompatible and do not elicit strong immune responses. When used as a surface coating on medical implants, it has been shown to improve outcomes without causing adverse effects. Systemic toxicity is not a primary concern as it is rapidly degraded; however, high systemic concentrations could theoretically cause bleeding by inhibiting platelet aggregation, which is a potential on-target toxicity.
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| 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.
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| Additional Infomation |
The RGD (Arg-Gly-Asp) peptide sequence was discovered as the minimal cell recognition domain in fibronectin. RGDC is one of the simplest RGD-containing peptides. The cysteine (Cys) residue at the C-terminus is not part of the recognition motif but is often included to allow for specific, site-directed conjugation to other molecules or surfaces through its thiol group. RGDC is a standard research chemical used in many fields, including cell adhesion studies, cancer research (to inhibit metastasis), tissue engineering (to improve scaffold cell adhesion), and drug delivery. The TFA salt form enhances solubility and stability. It is not an approved drug.
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| Molecular Formula |
C19H29F6N7O11S
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|---|---|
| Molecular Weight |
677.53
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| Exact Mass |
563.162
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| CAS # |
2171504-22-4
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| Related CAS # |
Arg-Gly-Asp-Cys;109292-46-8
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| PubChem CID |
168013180
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| Appearance |
Typically exists as solid at room temperature
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| Hydrogen Bond Donor Count |
10
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| Hydrogen Bond Acceptor Count |
15
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| Rotatable Bond Count |
14
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| Heavy Atom Count |
37
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| Complexity |
753
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| Defined Atom Stereocenter Count |
3
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| SMILES |
C(C[C@@H](C(=O)NCC(=O)N[C@H](CC(=O)O)C(=O)N[C@@H](CS)C(=O)O)N)CN=C(N)N.C(=O)(C(F)(F)F)O
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| InChi Key |
AJFGGKXZCJCXNM-HBJOHWKNSA-N
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| InChi Code |
InChI=1S/C15H27N7O7S.C2HF3O2/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;3-2(4,5)1(6)7/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);(H,6,7)/t7-,8+,9-;/m0./s1
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| Chemical Name |
(3R)-3-[[2-[[(2S)-2-amino-5-(diaminomethylideneamino)pentanoyl]amino]acetyl]amino]-4-[[(1R)-1-carboxy-2-sulfanylethyl]amino]-4-oxobutanoic acid;2,2,2-trifluoroacetic 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 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: 250 mg/mL
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (Infinity mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.4759 mL | 7.3797 mL | 14.7595 mL | |
| 5 mM | 0.2952 mL | 1.4759 mL | 2.9519 mL | |
| 10 mM | 0.1476 mL | 0.7380 mL | 1.4759 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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