| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 100mg | |||
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| Targets |
GRGDS targets integrin receptors, specifically αvβ3 and αvβ5. Integrins are cell surface receptors that mediate cell-extracellular matrix adhesion and signal transduction. By binding to these integrin receptors, GRGDS competitively inhibits the interaction between cells and extracellular matrix proteins such as fibronectin, thereby modulating cell adhesion and migration.
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| ln Vitro |
Gly-Arg-Gly-Asp-Ser has an IC50 of 5 μM when it comes to binding the integrin receptor αvβ3 [1]. TiO2 nanotubes immobilized with Gly-Arg-Gly-Asp-Ser boosted osteoblast-like cell (MG-63) adherence and markedly increased cell spreading and proliferation [2].
In vitro, GRGDS binds to integrin receptors αvβ3 and αvβ5 with estimated IC₅₀ values of approximately 5 μM and 6.5 μM, respectively. Immobilized GRGDS on titanium dioxide nanotubes significantly enhances osteoblast-like cell (MG-63) adhesion, spreading, and proliferation. The peptide also inhibits fibronectin binding to platelets, reducing the risk of metastasis in experimental models. |
| ln Vivo |
In vivo, GRGDS has been shown to inhibit metastasis in syngeneic mice or in mice lacking platelet function when co-injected with B16-F10 melanoma cells. The peptide is used in wound healing research, where GRGDS-functionalized biomaterials promote tissue repair by facilitating cell migration and adhesion at wound sites. It also plays a role in stem cell mobilization and harvesting procedures.
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| Enzyme Assay |
In vitro receptor binding assays for GRGDS are performed using radioligand competition binding techniques. The peptide is incubated with membranes expressing integrin receptors (αvβ3 or αvβ5) and a radiolabeled integrin ligand. The displacement of the radioligand is quantified to determine binding affinity, with IC₅₀ values calculated from competition curves.
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| Cell Assay |
In vitro cellular assays for GRGDS are performed using cell lines such as MG-63 osteoblast-like cells or fibroblasts. Cells are cultured on GRGDS-immobilized surfaces or treated with soluble GRGDS, and cell adhesion, spreading, and proliferation are assessed. Migration assays, such as Boyden chamber assays, are used to evaluate the peptide's effects on cell motility.
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| Animal Protocol |
In vivo animal experiments for GRGDS are conducted in mouse models. A typical protocol involves co-injection of GRGDS with B16-F10 melanoma cells into syngeneic mice, followed by assessment of metastasis formation. In wound healing studies, GRGDS-functionalized biomaterials are applied to skin wounds, and healing rates are monitored. Stem cell mobilization studies evaluate the effects of GRGDS on stem cell behavior during transplantation procedures.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of GRGDS have not been systematically characterized. The peptide has a molecular weight of 490.47 and molecular formula C₁₇H₃₀N₈O₉. It is supplied as a lyophilized powder with purity >96%. The peptide should be stored at -20°C or -80°C and freeze-thaw cycles should be avoided. It is soluble in water and DMSO.
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| Toxicity/Toxicokinetics |
Toxicological data for GRGDS are not extensively reported. As a research-use peptide, its safety profile has not been formally evaluated in comprehensive preclinical toxicology studies. The compound is intended for research purposes only and is not approved for human therapeutic use. Standard laboratory safety precautions should be followed when handling this peptide.
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| References |
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| Additional Infomation |
GRGDS is a synthetic pentapeptide with CAS number 96426-21-0, molecular formula C₁₇H₃₀N₈O₉, and molecular weight 490.47. The sequence is Gly-Arg-Gly-Asp-Ser. It is a cell-adhesive motif that binds to integrin receptors αvβ3 and αvβ5 with IC₅₀ values of ~5 and ~6.5 μM. GRGDS is used in cell adhesion, tissue engineering, and cancer metastasis research.
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| Molecular Formula |
C17H30N8O9
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|---|---|
| Molecular Weight |
490.4683
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| Exact Mass |
490.214
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| CAS # |
96426-21-0
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| Related CAS # |
Gly-Arg-Gly-Asp-Ser TFA;2828433-23-2
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| PubChem CID |
123811
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| Appearance |
White to off-white solid powder
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| Density |
1.66 g/cm3
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| Index of Refraction |
1.664
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| LogP |
-7.9
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| Hydrogen Bond Donor Count |
10
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
16
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| Heavy Atom Count |
34
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| Complexity |
785
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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](CO)C(=O)O)NC(=O)CN)CN=C(N)N
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| InChi Key |
RGNVSYKVCGAEHK-GUBZILKMSA-N
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| InChi Code |
InChI=1S/C17H30N8O9/c18-5-11(27)23-8(2-1-3-21-17(19)20)14(31)22-6-12(28)24-9(4-13(29)30)15(32)25-10(7-26)16(33)34/h8-10,26H,1-7,18H2,(H,22,31)(H,23,27)(H,24,28)(H,25,32)(H,29,30)(H,33,34)(H4,19,20,21)/t8-,9-,10-/m0/s1
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| Chemical Name |
(3S)-3-[[2-[[(2S)-2-[(2-aminoacetyl)amino]-5-(diaminomethylideneamino)pentanoyl]amino]acetyl]amino]-4-[[(1S)-1-carboxy-2-hydroxyethyl]amino]-4-oxobutanoic 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) |
DMSO : ~50 mg/mL (~101.94 mM)
H2O : ~33.33 mg/mL (~67.96 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.10 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.10 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.10 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (203.89 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0389 mL | 10.1943 mL | 20.3886 mL | |
| 5 mM | 0.4078 mL | 2.0389 mL | 4.0777 mL | |
| 10 mM | 0.2039 mL | 1.0194 mL | 2.0389 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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