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Cyclo(RGDyC) TFA

Cat No.:V86159 Purity: ≥98%
Cyclo(RGDyC) TFA
Cyclo(RGDyC) TFA Chemical Structure Product category: Peptides
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1mg
5mg
Other Sizes
Official Supplier of:
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Product Description
Cyclo(RGDyC) TFA is a cyclic pentapeptide with anti-angiogenic properties. Cyclo(RGDyC) TFA can be combined with liposome delivery systems for the study of ocular neovascular diseases and cancer.
Cyclo(RGDyC) TFA is a cyclic peptide containing the arginine-glycine-aspartic acid (RGD) motif, which is recognized by integrin receptors. The peptide sequence is cyclo(Arg-Gly-Asp-D-Tyr-Cys). It is supplied as a TFA salt. This compound is used as a targeting ligand for integrin αvβ3 and αvβ5, which are overexpressed on tumor endothelial cells and cancer cells.
Biological Activity I Assay Protocols (From Reference)
Targets
Cyclo(RGDyC) TFA targets integrin receptors, particularly αvβ3 and αvβ5. The RGD motif is the minimal peptide sequence recognized by these integrins. Integrin αvβ3 is overexpressed on activated endothelial cells during angiogenesis and on various cancer cells. By binding to these integrins, the peptide can be used to target tumor vasculature and cancer cells for diagnostic or therapeutic applications.
ln Vitro
In vitro, Cyclo(RGDyC) TFA is used as a targeting ligand to study integrin-mediated cell adhesion and signaling. The peptide binds to integrin αvβ3 and αvβ5 with high affinity. It can be used to block integrin-ligand interactions, to study integrin-mediated cellular processes such as angiogenesis, cell migration, and metastasis. The peptide is also used to functionalize nanoparticles or other delivery vehicles for targeted drug delivery.
ln Vivo
In vivo, Cyclo(RGDyC) TFA is used to target tumor vasculature and cancer cells expressing integrin αvβ3 and αvβ5. The peptide can be conjugated to imaging agents for tumor imaging or to therapeutic agents for targeted cancer therapy. Its cyclic structure provides enhanced stability and binding affinity compared to linear RGD peptides. The compound has been extensively studied in preclinical models of cancer.
Enzyme Assay
Non-cellular binding assays for Cyclo(RGDyC) TFA involve measuring its binding affinity to purified integrin αvβ3 or αvβ5 using techniques such as surface plasmon resonance (SPR), ELISA, or fluorescence polarization. The peptide's ability to inhibit integrin-ligand interactions can also be assessed using competitive binding assays. These assays confirm the peptide's high affinity and specificity for its integrin targets.
Cell Assay
In vitro cellular experiments with Cyclo(RGDyC) TFA are conducted in integrin-expressing cell lines. Cells are treated with the peptide, and integrin-mediated adhesion, migration, or signaling is assessed. The peptide can be used to block integrin-dependent processes such as cell attachment to extracellular matrix proteins. Fluorescently labeled versions of the peptide are used to study receptor binding and internalization by flow cytometry or fluorescence microscopy.
Animal Protocol
In vivo animal studies with Cyclo(RGDyC) TFA are performed in murine tumor models. The peptide is conjugated to imaging agents (e.g., fluorescent dyes, radionuclides) or therapeutic agents (e.g., drugs, nanoparticles) and administered intravenously. Tumor targeting is assessed by imaging or by measuring the accumulation of the conjugate in tumor tissue. Therapeutic efficacy is evaluated by monitoring tumor growth and survival.
ADME/Pharmacokinetics
Cyclo(RGDyC) TFA has the peptide sequence cyclo(Arg-Gly-Asp-D-Tyr-Cys). The TFA salt form enhances solubility. The compound is typically stored at -20°C and protected from light. It is soluble in water and aqueous buffers. Purity is typically ≥95%. The compound is for research use only and not for human therapeutic applications.
Toxicity/Toxicokinetics
Toxicity data for Cyclo(RGDyC) TFA are typically characterized as part of the safety evaluation of RGD peptide-based imaging or therapeutic agents. The peptide itself is generally well-tolerated. Standard toxicology studies assess the safety of the final conjugate. Researchers should consult the safety data sheet and handle the compound with appropriate laboratory safety precautions.
References

[1].Aqueous synthesized near-infrared-emitting quantum dots for RGD-based in vivo active tumour targeting. Nanotechnology. 2013 Apr 5;24(13):135101.

[2].Photostable and Biocompatible Fluorescent Silicon Nanoparticles-Based Theranostic Probes for Simultaneous Imaging and Treatment of Ocular Neovascularization. Anal Chem. 2018 Jul 3;90(13):8188-8195.

Additional Infomation
Cyclo(RGDyC) TFA is a cyclic RGD peptide targeting integrin αvβ3 and αvβ5. The peptide is used for tumor targeting, angiogenesis research, and the development of targeted diagnostic and therapeutic agents. All products are for research use only.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C24H34N8O8S.XC2HF3O2
Molecular Weight
594.64 (free base)
Appearance
White to off-white solid powder
HS Tariff Code
2934.99.9001
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)
Solubility Data
Solubility (In Vitro)
Typically soluble in DMSO (e.g. 10 mM)
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
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*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 : PEG300Tween 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).
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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)]
*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.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL 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).
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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders


Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Calculator

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What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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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