| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Transferrin receptor (TfR). TfR-T12 is a BBB-penetrated transferrin receptor-binding peptide that displays binding affinity in the nM range. Upon binding to TfR, the peptide is subsequently internalized into TfR-expressing cells via receptor-mediated endocytosis, enabling the delivery of conjugated therapeutic cargos across biological barriers.
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| ln Vitro |
TfR-T12 internalizes into TfR-expressing cells after binding to TfR[1]. Transferrin can bind to one site on TfRs, but TfR-T12, a synthetic peptide produced through phage display, can bind to another website. For the purpose of creating multifunctional lipid vesicles, TfR-T12 can be chemically conjugated with 3-(N-succinimidyloxyglutaryl)aminopropyl-polyethyleneglycol(2000)-carbamyl distearoyl phosphatidylethanolamine (NHS-PEG2000-DSPE)[2].
In vitro, TfR-T12 TFA binds to the transferrin receptor (TfR) on the surface of endothelial cells, showing high affinity in the nanomolar range. This binding facilitates the internalization of the peptide into cells via endocytosis, allowing it to act as a transport vehicle for conjugated molecules. The TFA (trifluoroacetic acid) salt form is used to enhance the peptide's stability and solubility. |
| ln Vivo |
In vivo, TfR-T12 TFA can penetrate the blood-brain barrier and has been used to deliver various therapeutic cargos, including proteins and nanoparticles, to the brain in animal models. This property makes it a valuable tool for researching treatments for neurological disorders. It serves as a control or targeting ligand in studies of drug delivery across the BBB.
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| Enzyme Assay |
Transferrin receptor binding assay: Membranes from cells expressing TfR are incubated with 125I-labeled transferrin or a fluorescent TfR probe and increasing concentrations of TfR-T12 TFA (0-1000 nM) in binding buffer (50 mM Tris-HCl, pH 7.4, 150 mM NaCl, 1% BSA) for 2 h at 4degC. Non-specific binding is determined with excess unlabeled transferrin. Bound radioactivity or fluorescence is measured, and IC50 is calculated.
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| Cell Assay |
Receptor-mediated internalization assay: TfR-expressing cells (e.g., bEnd.3 brain endothelial cells) are seeded in 6-well plates. Cells are incubated with fluorescently labeled TfR-T12 TFA (0.1-10 uM) or a conjugate thereof for 30-60 min at 37degC. After washing, cells are fixed and counterstained with DAPI for nuclei and WGA for membranes. Internalization is visualized by confocal microscopy and quantified by flow cytometry.
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| Animal Protocol |
BBB penetration model: C57BL/6 mice are injected intravenously with a fluorescently labeled TfR-T12 TFA conjugate (1-10 mg/kg). At 1, 4, and 24 h post-injection, brains and other organs are collected. Brain sections are examined by confocal microscopy to detect fluorescence in the brain parenchyma. Alternatively, the conjugated cargo (e.g., a therapeutic protein) is measured in brain homogenates by ELISA or LC-MS.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for the peptide alone are not detailed. As a peptide (MW 1604.75, TFA salt), it has a short plasma half-life (minutes) due to proteolytic degradation and is administered via intravenous or intraperitoneal injection. The TFA salt enhances solubility in aqueous buffers, enabling effective conjugation and formulation for in vivo delivery.
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| Toxicity/Toxicokinetics |
Toxicity data for TfR-T12 TFA are limited. As a peptide targeting the transferrin receptor, it is generally well-tolerated at effective concentrations. At high doses, saturation of the TfR pathway could potentially interfere with iron homeostasis. It is intended for research use only and not for human therapeutic applications. Standard peptide handling precautions should be followed.
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| References |
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| Additional Infomation |
TfR-T12 TFA is a research tool for targeted drug delivery across the BBB and to TfR-expressing tumors. It is not a therapeutic agent and has not been approved for clinical use. The peptide was initially identified via phage display for its selectivity and internalization properties. It can be conjugated to various cargos (e.g., nanoparticles, antibodies) for delivery studies. For research use only.
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| Molecular Formula |
C73H100F3N19O17S
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|---|---|
| Molecular Weight |
1604.75
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| Related CAS # |
TfR-T12;344618-30-0
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| Appearance |
White to off-white 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 (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 (~62.32 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 | 0.6232 mL | 3.1158 mL | 6.2315 mL | |
| 5 mM | 0.1246 mL | 0.6232 mL | 1.2463 mL | |
| 10 mM | 0.0623 mL | 0.3116 mL | 0.6232 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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