| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Integrin[1]
Integrins. RGD Trifluoroacetate binds to multiple integrin subtypes including alpha3beta1, alpha5beta1, alpha8beta1, alphaIIbbeta3, alphavbeta1, alphavbeta3, alphavbeta5, alphavbeta6, alphavbeta8, and to some extent alpha2beta1 and alpha4beta1. These are the 24 integrins that bind to extracellular matrix (ECM) molecules in an RGD-dependent manner. By binding to integrins on cell surfaces, this tripeptide mediates cell adhesion, migration, and signaling. |
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| ln Vitro |
For enhanced cell attachment on synthetic surfaces, RGD Trifluoroacetate is the most popular and successful peptide sequence. α3β1, α5β1, α8β1, αIIbβ3, αvβ1, αvβ3, αvβ5, αvβ6, αvβ8, and to some extent α2β1 and α4β1 are the 24 integrins that bind to ECM molecules in an RGD dependent manner[1].
In vitro, RGD Trifluoroacetate is used for enhanced cell attachment on synthetic surfaces, where it is the most effective and frequently employed peptide sequence. It enables specific cellular responses by localizing to particular cell lines through integrin binding. The peptide facilitates cell adhesion and serves as a critical tool for studying integrin-ligand interactions and promoting cell attachment on biomaterial surfaces in tissue engineering and drug delivery applications. |
| ln Vivo |
Direct in vivo activity of RGD Trifluoroacetate itself is not extensively reported, as it is primarily used as a surface coating or conjugation tool. However, RGD peptides in general have been shown to influence cell behavior and tissue integration in vivo when immobilized on biomaterial surfaces. The compound facilitates cell adhesion and can promote targeted delivery of therapeutics when conjugated to nanoparticles or drug carriers due to its integrin-binding properties. Further in vivo studies would be required to establish specific efficacy.
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| Enzyme Assay |
The binding affinity of RGD Trifluoroacetate to integrin receptors can be assessed using surface plasmon resonance (SPR) or enzyme-linked immunosorbent assay (ELISA). For SPR, immobilize purified integrin protein on a sensor chip, then flow increasing concentrations of RGD Trifluoroacetate (e.g., 0.1-100 uM) over the chip in running buffer (PBS with 0.005% Tween-20, pH 7.4) at 25degC. Calculate binding affinity (KD) from the association and dissociation rates. For competitive ELISA, coat wells with ECM protein, incubate with integrin in the presence of varying RGD concentrations, and measure bound integrin using specific antibodies.
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| Cell Assay |
Culture adherent cells (e.g., fibroblasts or endothelial cells) in 96-well plates at 37degC with 5% CO2 until 70-80% confluent. For cell adhesion assays, coat plates with RGD Trifluoroacetate (0.1-100 ug/mL) in PBS overnight at 4degC, then block with 1% BSA. Seed cells (1-5×10⁴ cells/well) and incubate for 30-60 min at 37degC. Wash away non-adherent cells, fix with 4% paraformaldehyde, and stain with crystal violet or Calcein-AM. Quantify adhesion by measuring absorbance or fluorescence. For cell spreading studies, visualize actin cytoskeleton using phalloidin staining.
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| Animal Protocol |
For in vivo studies using RGD-functionalized biomaterials or drug delivery systems, use immunocompromised mice (e.g., nude mice, 6-8 weeks old, 18-22 g) bearing subcutaneous xenograft tumors. Administer RGD-conjugated nanoparticles or therapeutics intravenously via tail vein at doses determined from preliminary efficacy studies (typically 1-10 mg/kg equivalent of the RGD peptide), once every 2-3 days for 2-4 weeks. Monitor tumor volume using calipers every 2-3 days and body weight twice weekly. Collect blood at multiple time points for pharmacokinetic analysis and harvest tumors and major organs at study endpoint for biodistribution analysis.
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| ADME/Pharmacokinetics |
Detailed ADME properties specific to RGD Trifluoroacetate are not extensively characterized. As a tripeptide, it is likely to undergo rapid degradation by proteases in biological fluids, which limits its systemic bioavailability when administered alone. However, when conjugated to nanoparticles or larger carriers, the pharmacokinetic profile is dominated by the carrier. The trifluoroacetate salt form enhances solubility and stability. The compound is soluble in water at ≥ 60 mg/mL (130.33 mM). It should be stored as a powder at -20degC for up to 3 years and in solvent at -80degC for 6 months.
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| Toxicity/Toxicokinetics |
The safety profile of RGD Trifluoroacetate is generally considered favorable for research use. The compound should be handled with standard laboratory precautions: use personal protective equipment including gloves and lab coat, avoid inhalation and skin contact. Based on its peptide nature, acute toxicity is expected to be low at typical research concentrations. However, as with all research chemicals, it should be handled with care. The compound is for research use only and not intended for diagnostic or therapeutic use in humans or animals. No teratogenic or carcinogenic effects have been reported for this specific salt form.
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| References | |
| Additional Infomation |
RGD Trifluoroacetate is exclusively a research reagent used as a building block for studying cell adhesion and integrin interactions. It has no direct clinical use. Its primary applications include: 1) Coating of biomaterials and tissue engineering scaffolds to promote cell attachment; 2) Conjugation to nanoparticles for targeted drug delivery to integrin-expressing cells; 3) Studying integrin-mediated signaling pathways; 4) As a standard control in cell adhesion assays. It is not approved for therapeutic use. The RGD sequence is found in many extracellular matrix proteins and serves as a recognition motif for integrin binding.
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| Molecular Formula |
C14H23F3N6O8
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|---|---|
| Molecular Weight |
460.363033533096
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| Exact Mass |
460.152
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| CAS # |
2378808-45-6
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| Related CAS # |
RGD;99896-85-2
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| PubChem CID |
132472231
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
8
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| Hydrogen Bond Acceptor Count |
13
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
31
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| Complexity |
588
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| Defined Atom Stereocenter Count |
2
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| SMILES |
FC(C(=O)O)(F)F.O=C([C@H](CCC/N=C(\N)/N)N)NCC(N[C@H](C(=O)O)CC(=O)O)=O
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| InChi Key |
FBPDETPEHPAQDC-LEUCUCNGSA-N
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| InChi Code |
InChI=1S/C12H22N6O6.C2HF3O2/c13-6(2-1-3-16-12(14)15)10(22)17-5-8(19)18-7(11(23)24)4-9(20)21;3-2(4,5)1(6)7/h6-7H,1-5,13H2,(H,17,22)(H,18,19)(H,20,21)(H,23,24)(H4,14,15,16);(H,6,7)/t6-,7-;/m0./s1
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| Chemical Name |
(2S)-2-[[2-[[(2S)-2-amino-5-(diaminomethylideneamino)pentanoyl]amino]acetyl]amino]butanedioic acid;2,2,2-trifluoroacetic 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) |
H2O : ≥ 60 mg/mL (130.33 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (217.22 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 | 2.1722 mL | 10.8611 mL | 21.7221 mL | |
| 5 mM | 0.4344 mL | 2.1722 mL | 4.3444 mL | |
| 10 mM | 0.2172 mL | 1.0861 mL | 2.1722 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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