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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| Targets |
GRGDSP targets integrins, a family of cell surface receptors that mediate cell adhesion to the extracellular matrix (ECM). The RGD (Arg-Gly-Asp) sequence is a well-known integrin recognition motif found in many ECM proteins, including fibronectin. By mimicking this sequence, GRGDSP competes with native ECM proteins for integrin binding, thereby inhibiting integrin-mediated cell adhesion, migration, and signaling.
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| ln Vitro |
GRGDSP (Gly-Arg-Gly-Asp-Ser-Pro integrin inhibitor, containing RGD-peptide) has been shown to be infused transarterially. As a synthesized linear RGD peptide, GRGDSP (Gly-Arg-Gly-Asp-Ser-Pro) can prevent tumor cells from adhering to vascular endothelial cells and prevent them from spreading [1]. Gly-Arg-Gly-Asp-Ser-Pro, or GRGDSP, is a soluble RGD peptide that blocks integrins. In integrin research, GRGDSP and other RGD peptides are frequently utilized. In order to encourage endothelialization, GRGDSP can be applied to the surface of cardiovascular implants, such as vascular grafts [2].
In vitro, GRGDSP effectively blocks integrin-mediated cell adhesion. It is used as a soluble integrin-blocking peptide in cell adhesion assays. By inhibiting tumor cell adhesion to vascular endothelial cells, it can prevent the spread of cancer cells. It is also used to study the role of integrins in various cellular processes, including migration, proliferation, and survival. |
| ln Vivo |
In vivo, GRGDSP is used to modify the surface of cardiovascular implants, such as vascular grafts. By promoting endothelialization, it helps to create a non-thrombogenic surface and improve the long-term performance of the implant. It has also been investigated for its potential in treating hepatocellular carcinoma (HCC) by inhibiting tumor cell adhesion and limiting metastasis.
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| Enzyme Assay |
The in vitro integrin binding assay for GRGDSP involves measuring its ability to inhibit the binding of cells to immobilized ECM proteins, such as fibronectin or vitronectin. Cells are pre-incubated with varying concentrations of the peptide and then allowed to adhere to ECM-coated surfaces. The number of adherent cells is quantified, and the IC50 is calculated. Alternatively, a competitive binding assay using a labeled ligand can be used.
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| Cell Assay |
In vitro cell culture studies for GRGDSP utilize cancer cell lines, such as hepatocellular carcinoma (HCC) cells, to study its effect on cell adhesion and migration. Cells are treated with the peptide, and their ability to adhere to ECM-coated surfaces or to migrate through a porous membrane (Boyden chamber assay) is assessed. The expression of integrins and downstream signaling molecules is analyzed by Western blotting.
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| Animal Protocol |
In vivo animal experiments for GRGDSP are performed in models of cancer metastasis or in models of vascular graft implantation. In the metastasis model, the peptide is administered systemically, and the number of metastatic foci in the lungs or liver is counted. In the vascular graft model, the graft is coated with the peptide, and endothelialization is assessed by histology or by scanning electron microscopy.
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| ADME/Pharmacokinetics |
GRGDSP is a peptide with a molecular formula of C22H37N9O10 and a molecular weight of 587.58 g/mol. It is a lyophilized powder that is soluble in water and aqueous buffers. It is typically stored as a powder at -20°C for long-term stability. Its stability is maintained under recommended storage conditions. It is a white or off-white lyophilized powder.
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| Toxicity/Toxicokinetics |
Toxicological data for GRGDSP are limited, as it is a research compound. As a peptide, it is expected to have low toxicity. It is not intended for human therapeutic use. Standard safety precautions for handling peptides should be followed.
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| References |
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| Additional Infomation |
See also: glycyl-arginyl-glycyl-aspartyl-seryl-proline (note moved to).
GRGDSP is a research compound with no clinical approval. It is a valuable tool for studying integrin biology and the role of integrins in cell adhesion, migration, and cancer metastasis. It is also used in the development of biomaterials for cardiovascular implants to improve their biocompatibility and endothelialization. It serves as a standard for RGD-containing peptides in various research applications. |
| Molecular Formula |
C22H37N9O10
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| Molecular Weight |
587.58348441124
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| Exact Mass |
587.266
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| CAS # |
91037-75-1
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| Related CAS # |
GRGDSP TFA
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| PubChem CID |
492973
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| Appearance |
White to off-white solid powder
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| LogP |
-7.9
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| Hydrogen Bond Donor Count |
10
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
17
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| Heavy Atom Count |
41
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| Complexity |
1020
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| Defined Atom Stereocenter Count |
4
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| SMILES |
C1C[C@H](N(C1)C(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)CNC(=O)[C@H](CCCN=C(N)N)NC(=O)CN)C(=O)O
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| InChi Key |
NTEDOEBWPRVVSG-XUXIUFHCSA-N
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| InChi Code |
InChI=1S/C22H37N9O10/c23-8-15(33)28-11(3-1-5-26-22(24)25)18(37)27-9-16(34)29-12(7-17(35)36)19(38)30-13(10-32)20(39)31-6-2-4-14(31)21(40)41/h11-14,32H,1-10,23H2,(H,27,37)(H,28,33)(H,29,34)(H,30,38)(H,35,36)(H,40,41)(H4,24,25,26)/t11-,12-,13-,14-/m0/s1
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| Chemical Name |
(2S)-1-[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[(2-aminoacetyl)amino]-5-(diaminomethylideneamino)pentanoyl]amino]acetyl]amino]-3-carboxypropanoyl]amino]-3-hydroxypropanoyl]pyrrolidine-2-carboxylic 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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 : ~100 mg/mL (~170.19 mM)
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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 | 1.7019 mL | 8.5095 mL | 17.0190 mL | |
| 5 mM | 0.3404 mL | 1.7019 mL | 3.4038 mL | |
| 10 mM | 0.1702 mL | 0.8509 mL | 1.7019 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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