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Purity: ≥98%
RGD (Arg-Gly-Asp) is a tripeptide that is the most common peptide motif responsible for cell adhesion to the ECM-extracellular matrix. It acts by mimicking cell adhesion proteins and binding to integrins. RGD peptide can also promote apoptosis through activation of conformation changes enhancing pro-caspase-3 activation and autoprocessing. Cell adhesion proteins called integrins recognize and bind to this sequence, which is found within many matrix proteins, including fibronectin, fibrinogen, vitronectin, osteopontin, and several other adhesive extracellular matrix proteins
| Targets |
RGD (Arg-Gly-Asp) specifically binds to integrin receptors αVβ3 and αVβ5, mediating cell adhesion and signaling pathways [1]
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| ln Vitro |
The most popular and successful peptide sequence for promoting cell attachment on artificial surfaces is RGD. 24 integrins—α3β1, α5β1, α8β1, αIIbβ3, αvβ1, αvβ3, αvβ5, αvβ6, αvβ8, and, to a lesser extent, α2β1 and α4β1—bind to ECM molecules in an RGD-dependent manner[1].
RGD-modified polymers significantly enhanced endothelial cell (HUVEC) adhesion and spreading on biomaterial surfaces, with cell density increasing by 3- to 5-fold compared to unmodified controls [1] RGD-functionalized surfaces promoted focal adhesion formation and actin cytoskeleton organization in fibroblasts, as visualized by immunofluorescence staining for vinculin and phalloidin [1] RGD-containing peptides induced dose-dependent adhesion of melanoma cells (B16F10) to extracellular matrix proteins (e.g., fibronectin), with maximal adhesion at 10 μM peptide concentration [1] RGD-modified poly(lactic-co-glycolic acid) (PLGA) scaffolds supported osteoblast differentiation, as indicated by increased alkaline phosphatase activity and collagen type I deposition [1] |
| ln Vivo |
Anima study suggested that the RGD-4C-FITC-peptide bound to both endothelial and tumor cells in vivo and that peptide targeting should allow the delivery of therapeutic drugs to both endothelial and tumor cells.
RGD-coated titanium implants showed improved osseointegration in rat femoral defect models, with new bone formation increasing by 40% compared to uncoated implants after 8 weeks [1] RGD-modified hydrogels promoted neovascularization in a murine subcutaneous model, as demonstrated by CD31 immunohistochemistry revealing a 2.5-fold increase in microvessel density [1] |
| Enzyme Assay |
Integrin binding assay: Biotinylated RGD peptides were immobilized on streptavidin-coated plates. Recombinant αVβ3 integrin (100 nM) was added, and binding was detected using anti-αV antibody-conjugated horseradish peroxidase (HRP). Absorbance at 450 nm indicated dose-dependent binding, with maximal signal at 5 μM RGD [1]
- Focal adhesion kinase (FAK) activation assay: HUVECs seeded on RGD-modified surfaces were lysed after 2 hours, and phosphorylated FAK (Tyr397) levels were quantified by Western blot. RGD treatment increased p-FAK expression by 200% compared to non-adherent controls [1] |
| Cell Assay |
Cell adhesion assay: Cells (e.g., HUVECs, fibroblasts) were suspended in serum-free medium containing RGD peptides (0.1–100 μM) and seeded onto polymer surfaces. After 1 hour, non-adherent cells were removed by washing, and adherent cells were stained with crystal violet. Absorbance at 595 nm was used to quantify adhesion efficiency [1]
- Migration assay: A scratch wound was created in confluent HUVEC monolayers cultured on RGD-modified plates. Cells were allowed to migrate for 24 hours, and wound closure was measured by phase-contrast microscopy. RGD-coated surfaces enhanced migration by 30% compared to unmodified controls [1] - Differentiation assay: Osteoblast precursor cells (MC3T3-E1) cultured on RGD-functionalized scaffolds showed increased mineralization after 21 days, as assessed by alizarin red staining and calcium deposition quantification [1] |
| Animal Protocol |
Osseointegration study: Titanium implants coated with RGD-grafted poly(ethylene glycol) (PEG) were inserted into rat femoral condyles. Animals were sacrificed at 4 and 8 weeks, and implants were analyzed by micro-computed tomography (μCT) and histology. RGD-treated groups exhibited higher bone-implant contact (BIC) percentages (55% vs. 30% in controls) [1]
- Neovascularization assay: RGD-modified gelatin hydrogels were implanted subcutaneously in C57BL/6 mice. After 7 days, implants were harvested, fixed, and stained for CD31 to visualize endothelial cells. Microvessel density was quantified using ImageJ software [1] |
| Toxicity/Toxicokinetics |
RGD-modified biomaterials showed no signs of cytotoxicity or inflammatory response in vitro (MTT assay) or in vivo (histopathological analysis) [1]
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| References | |
| Additional Infomation |
Arg-Gly-Asp is an oligopeptide. Arginyl-glycyl-aspartic acid has been reported in Bitis arietans, and relevant data are available. RGD sequences are key motifs mediating cell-matrix interactions via extracellular matrix proteins [1]. RGD-based biomaterials can be used in tissue engineering, drug delivery, and implant coatings [1]. The bioactivity of RGDs depends on their presentation (e.g., surface density, peptide conformation) and the specific integrin isoform expressed by the target cells [1]. RGD-modified polymers can be tailored to promote cell-specific adhesion while minimizing nonspecific protein adsorption [1].
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| Molecular Formula |
C12H22N6O6
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| Molecular Weight |
346.34
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| Exact Mass |
346.16
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| CAS # |
99896-85-2
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| Related CAS # |
RGD Trifluoroacetate;2378808-45-6
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| PubChem CID |
104802
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| Appearance |
White to off-white solid powder
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| Density |
1.6±0.1 g/cm3
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| Melting Point |
153-155℃ (ethyl ether )
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| Index of Refraction |
1.648
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| LogP |
-1.94
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| Hydrogen Bond Donor Count |
7
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
24
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| Complexity |
504
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C(C[C@@H](C(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)O)N)CN=C(N)N
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| InChi Key |
IYMAXBFPHPZYIK-BQBZGAKWSA-N
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| InChi Code |
IYMAXBFPHPZYIK-BQBZGAKWSA-N
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| Chemical Name |
Arginylglycylaspartic acid
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| Synonyms |
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
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| 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) |
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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 | 2.8873 mL | 14.4367 mL | 28.8734 mL | |
| 5 mM | 0.5775 mL | 2.8873 mL | 5.7747 mL | |
| 10 mM | 0.2887 mL | 1.4437 mL | 2.8873 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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