Quick summary
RGDS (Arg-Gly-Asp-Ser) is the prototype integrin-binding tetrapeptide derived from fibronectin. It is the foundational tool in cell adhesion research and biomaterials surface functionalization, and its pharmacophore inspired FDA-approved antithrombotic drugs eptifibatide and tirofiban.
Overview
RGDS (Arg-Gly-Asp-Ser) is the prototype integrin-binding tetrapeptide sequence derived from fibronectin. It is the minimal consensus motif recognized by multiple integrin receptors and serves as the foundational tool peptide in cell adhesion, biomaterials surface functionalization, and integrin pharmacology research.
Mechanism of action
RGDS competes with extracellular matrix proteins (fibronectin, vitronectin, fibrinogen) for binding to integrin receptors — particularly αvβ3, αvβ5, α5β1, and αIIbβ3. The Asp residue forms a key salt bridge with the integrin metal ion-dependent adhesion site (MIDAS), while Arg contributes electrostatic interactions. In solution, RGDS acts as a competitive antagonist of cell-matrix adhesion. When tethered to biomaterial surfaces, it promotes controlled cell attachment. The Ser residue at the C-terminus confers selectivity for certain integrin subtypes compared to RGD alone.
Dosing protocols
| Purpose | Route | Dosage | Frequency | Notes |
|---|---|---|---|---|
| biomaterial surface functionalization | topical | 0–0 nmol/cm² | surface coating (single application) | Density typically 0.001–10 nmol/cm² depending on desired cell adhesion level; optimized empirically per system |
| integrin inhibition assay | intravenous | 10–1000 mcg/mL | research use only |
Dosing information is for educational purposes only. Consult a qualified healthcare professional before using any peptide.
Research summary
RGDS has been foundational to integrin biology since Pierschbacher and Ruoslahti defined the RGD sequence in fibronectin in 1984. It is widely used to functionalize hydrogels, scaffolds, and nanoparticles for tissue engineering. Soluble RGDS has been studied as an antiplatelet agent (αIIbβ3 antagonist). Countless biomaterial studies use RGDS density to tune cell adhesion, spreading, and fate. No clinical drug development has advanced RGDS itself, but structural analogs (eptifibatide, tirofiban) are FDA-approved antithrombotics based on RGD pharmacophore.[1][2][3][4]
Evidence grading
Each claimed benefit is graded by the strength of available evidence. Grades reflect study quality, not effect size.
Strong = multiple RCTs · Moderate = limited trials or observational · Preliminary = animal or in vitro only · Insufficient = anecdotal or no published data
Side effects
Side effects vary by individual. This is not an exhaustive list. Report unusual symptoms to a healthcare professional.
Common stacks
Peptides commonly paired with RGDS for synergistic effects.
Legal status
RGDS is a research peptide used in laboratory and biomaterials science contexts. It is not approved for human therapeutic use. Available from peptide suppliers as a research reagent.
Sourcing & access
Research compound
RGDS is classified as a research compound. Regulatory status varies by jurisdiction. Always verify current legal status and source from vendors providing third-party certificates of analysis (COA).
Frequently asked questions
RGDS (Arg-Gly-Asp-Ser) is a tetrapeptide representing the minimal consensus motif recognized by multiple integrin receptors. Derived from fibronectin, it is the foundational tool peptide in cell adhesion research, biomaterials science, and integrin pharmacology.
RGDS competes with extracellular matrix proteins for binding to integrin receptors including alpha-v-beta-3, alpha-5-beta-1, and alpha-IIb-beta-3. The Asp residue forms a key salt bridge with the integrin MIDAS domain. In solution it acts as a competitive adhesion antagonist; when tethered to surfaces it promotes controlled cell attachment.
RGDS itself is a research reagent not approved for human therapeutic use. However, structural analogs based on the RGD pharmacophore (eptifibatide and tirofiban) are FDA-approved antithrombotic drugs that block platelet aggregation by inhibiting integrin alpha-IIb-beta-3.
RGDS is widely used to functionalize hydrogels, scaffolds, and nanoparticles for tissue engineering. It is also used in integrin inhibition assays, platelet aggregation studies, and as a tool to tune cell adhesion density on biomaterial surfaces.
Research references
- RGDS peptide as an integrin antagonist: platelet aggregation inhibitionPubMed
- RGD peptide-integrin interactions: cell adhesion and biomaterial designPubMed
- RGDS and cyclic RGD peptides: selectivity for integrin subtypes and therapeutic usesPubMed
- RGD motifs in hydrogel scaffolds for tissue engineering: integrin-mediated cell behaviorPubMed