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| 1mg |
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| 5mg |
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| Targets |
Cyclo(Arg-Ala-Asp-(D-Tyr)-Lys) TFA is a control peptide for c(RGDyK) and does not target integrin receptors. The active c(RGDyK) peptide targets αvβ₃ and αvβ₅ integrins, which are involved in cell adhesion, angiogenesis, and tumor metastasis. The control peptide c(RADyK) substitutes alanine for glycine in the RGD motif, disrupting integrin binding while maintaining similar physicochemical properties.
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| ln Vitro |
As a control peptide for c(RGDyK), Cyclo(Arg-Ala-Asp-(D-Tyr)-Lys) TFA does not exhibit significant integrin-binding activity in vitro. While the active c(RGDyK) peptide binds to αvβ₃ integrin with high affinity (nM range), the RAD-substituted control shows minimal or no binding to integrin receptors, making it an ideal negative control for integrin-targeting studies.
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| ln Vivo |
As a control peptide, Cyclo(Arg-Ala-Asp-(D-Tyr)-Lys) TFA does not exhibit the in vivo activity associated with integrin-targeting RGD peptides. While c(RGDyK) shows tumor-targeting properties and anti-angiogenic activity in vivo, the RAD control peptide serves as a negative control to demonstrate the specificity of RGD-mediated targeting in animal models.
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| Enzyme Assay |
Non-cell-based binding assays for Cyclo(Arg-Ala-Asp-(D-Tyr)-Lys) TFA typically involve surface plasmon resonance (SPR) or enzyme-linked immunosorbent assay (ELISA) to confirm lack of integrin binding. A typical protocol includes: immobilizing integrin protein (αvβ₃ or αvβ₅) on a sensor chip or plate, flowing the peptide at various concentrations, and measuring binding response. The RAD peptide should show no significant binding compared to the RGD peptide.
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| Cell Assay |
Cellular assays with Cyclo(Arg-Ala-Asp-(D-Tyr)-Lys) TFA typically involve cell adhesion or competition assays. A representative protocol includes: culturing integrin-expressing cells (e.g., endothelial cells or cancer cells), coating plates with integrin ligands (e.g., vitronectin or fibronectin), pre-incubating cells with the RAD peptide or RGD peptide as control, and measuring cell adhesion. The RAD peptide should not inhibit cell adhesion, confirming specificity.
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| Animal Protocol |
In vivo animal studies with Cyclo(Arg-Ala-Asp-(D-Tyr)-Lys) TFA typically involve tumor-bearing mouse models to demonstrate specificity of RGD-mediated tumor targeting. A representative protocol includes: injecting fluorescently- or radio-labeled RGD peptide and RAD control peptide into mice bearing integrin-expressing tumors, performing imaging or biodistribution analysis, and comparing tumor accumulation between the RGD and RAD probes.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Cyclo(Arg-Ala-Asp-(D-Tyr)-Lys) TFA as a control peptide are similar to those of c(RGDyK). Typical PK parameters for cyclic RGD peptides include rapid clearance from circulation (t₁/₂ of 10–30 minutes), distribution primarily to kidneys and tumors, and renal excretion. The RAD control peptide is expected to have similar PK properties but without specific tumor targeting.
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| Toxicity/Toxicokinetics |
As a research-use peptide, Cyclo(Arg-Ala-Asp-(D-Tyr)-Lys) TFA is not intended for human therapeutic use. Toxicological data are limited. Standard safety precautions should be followed when handling the peptide. The compound should be stored in a sealed container, protected from moisture and light. Powder can be stored at -80°C for 2 years or -20°C for 1 year.
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| References | |
| Additional Infomation |
Cyclo(Arg-Ala-Asp-(D-Tyr)-Lys) TFA (c(RADyK) TFA) is an essential negative control for integrin-targeting research. The substitution of alanine for glycine in the RGD motif (RAD vs RGD) abolishes integrin binding while maintaining the cyclic structure and overall physicochemical properties of the peptide. This control is widely used in studies of angiogenesis, tumor targeting, and molecular imaging to validate the specificity of RGD-based probes.
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| Molecular Formula |
C28H43N9O8.XC2HF3O2
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| Molecular Weight |
633.70 (free acid)
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| Appearance |
Typically exists as solid at room temperature
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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
DMSO :~50 mg/mL (with sonication) |
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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.) |
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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