| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
α5β1
RGD peptide (GRGDNP) TFA targets integrin‑ligand interactions, competitively blocking the binding of α5β1 integrin to the extracellular matrix (ECM). The RGD motif is recognized by multiple integrins, but GRGDNP shows preferential activity against α5β1. By disrupting integrin‑mediated adhesion, the peptide induces apoptosis through conformational changes that enhance pro‑caspase‑3 activation and autoprocessing. |
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| ln Vitro |
The application of RGD peptide (GRGDNP) TFA (50 μM) eliminated the stretch-induced activation of IKK and IL-6 mRNA expression after a 3-hour preincubation period. In unstretched HUVECs, it has minimal impact on IL-6 mRNA expression and IKK activity[2]. Complete reversal of increased FN1 expression was observed in oxygen-glucose deprivation (OGD)-treated primary hippocampal neurons, HT22 cell lines, and their sEVs after 6 hours of treatment with RGD peptide (GRGDNP) TFA (300 μg/mL) [3].
In vitro, RGD peptide (GRGDNP) TFA (50 μM) eliminates stretch‑induced activation of IKK and IL‑6 mRNA expression in HUVECs after a 3‑hour preincubation period. It effectively disrupts cell‑ECM adhesion, leading to inhibited cell migration and induction of apoptosis. The peptide induces endothelin‑dependent vasoconstriction via α5β1, while αvβ3‑preferring peptides may not trigger this ex vivo response. Its role in regulating cell adhesion, migration, growth, and differentiation has been well documented. |
| ln Vivo |
In vivo, linear RGD peptides such as GRGDNP undergo rapid proteolytic degradation, with a half‑life typically less than 10 minutes, severely limiting their utility beyond short‑term cell adhesion assays. Despite this limitation, they are widely used in vitro and in vivo to study angiogenesis, tumor metastasis, and mechanisms of anoikis in cancer research. Cyclic RGD analogs have been developed to overcome the rapid proteolysis of linear peptides.
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| Enzyme Assay |
Non‑cellular binding assays for RGD peptide (GRGDNP) TFA involve measuring its ability to inhibit integrin‑ligand interactions. These assays can be performed using ELISA‑based competition assays where the peptide is incubated with purified integrin (e.g., α5β1) and immobilized ECM proteins. The inhibition of binding is quantified, and IC50 values are determined from dose‑response curves. Surface plasmon resonance (SPR) can also be employed to measure direct binding kinetics between the peptide and integrin.
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| Cell Assay |
In vitro cellular assays for RGD peptide (GRGDNP) TFA are performed using various cell types, including HUVECs and cancer cell lines. Cells are treated with the peptide (e.g., 50 μM for 3 hours), and the effects on integrin‑mediated signaling, cell adhesion, migration, and apoptosis are assessed. Cell adhesion assays measure the ability of cells to attach to ECM‑coated surfaces in the presence of the peptide. Migration is assessed using wound healing or transwell assays, and apoptosis is measured by caspase activation assays.
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| Animal Protocol |
In vivo animal experiments for RGD peptide (GRGDNP) TFA are limited due to the rapid proteolytic degradation of linear RGD peptides, which typically have a half‑life of less than 10 minutes in vivo. Despite this, the peptide has been used in short‑term models to study angiogenesis and tumor metastasis. For longer‑term studies, cyclic RGD analogs or peptide conjugates with improved stability are typically employed.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties for RGD peptide (GRGDNP) TFA are characterized by rapid proteolytic degradation in vivo, with a half‑life typically less than 10 minutes for linear RGD peptides. The compound has a molecular weight of 728.63 and a molecular formula of C25H39F3N10O12. It is soluble in DMSO (≥50 mg/mL) and should be stored as a powder at -20°C for up to 1 year. The TFA salt form enhances aqueous solubility for research applications.
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| Toxicity/Toxicokinetics |
Toxicological data for RGD peptide (GRGDNP) TFA are not extensively detailed in available sources. As a peptide that disrupts integrin‑mediated cell adhesion, it may have effects on normal tissue homeostasis. However, it is primarily used as a research tool at concentrations that are generally well‑tolerated in vitro and in short‑term in vivo models. Comprehensive toxicological profiling would be required for any therapeutic development.
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| References |
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| Additional Infomation |
RGD peptide (GRGDNP) TFA has a molecular weight of 728.63 and a molecular formula of C25H39F3N10O12. The sequence is Gly‑Arg‑Gly‑Asp‑Asn‑Pro (GRGDNP). It is a white to off‑white solid powder, soluble in DMSO (≥50 mg/mL). It functions as an inhibitor of integrin‑ligand interactions, competitively blocking α5β1's interaction with the extracellular matrix (ECM) and promoting apoptosis. It is supplied for research purposes only and is not approved for clinical use.
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| Molecular Formula |
C25H39F3N10O12
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|---|---|
| Molecular Weight |
728.63
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| Related CAS # |
RGD peptide (GRGDNP);114681-65-1
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| Appearance |
Solid powder
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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 :≥ 50 mg/mL (~68.62 mM)
DMSO :≥ 50 mg/mL (~68.62 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (137.24 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 | 1.3724 mL | 6.8622 mL | 13.7244 mL | |
| 5 mM | 0.2745 mL | 1.3724 mL | 2.7449 mL | |
| 10 mM | 0.1372 mL | 0.6862 mL | 1.3724 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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