| Size | Price | |
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| 1mg | ||
| 5mg | ||
| 10mg | ||
| Other Sizes |
| Targets |
No specific receptor. TAT peptide interacts electrostatically with negatively charged cell surface components such as heparan sulfate proteoglycans, phospholipids, and glycosaminoglycans. This interaction triggers endocytosis (macropinocytosis, clathrin-mediated) and/or direct membrane translocation, leading to efficient cellular internalization without significant toxicity.
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| ln Vitro |
The trans-activating transcriptional activator (Tat) from HIV-1 is the source of the cell-penetrating peptide known as TAT peptide (GRKKRRQRRRPQ)[1]. Because TAT peptide (GRKKRRQRRRPQ) functionalized hybrid nanoparticles combine optical detection and magnetic enrichment for quick and easy cell labeling, they are also being explored. An
In vitro, TAT peptide (0.1-10 uM) efficiently delivers conjugated cargoes into almost all cell types. It is used to study intracellular pathways, deliver therapeutic proteins, and transduce cells with nucleic acids. The peptide retains its transduction activity after covalent or non-covalent complexation with cargo, making it a versatile tool for basic research. |
| ln Vivo |
In vivo, TAT peptide has been used to deliver functional proteins, peptides, and antisense oligonucleotides to various organs, including the brain, after systemic administration. It crosses the blood-brain barrier and can target intracellular compartments. It serves as a research tool for studying potential therapeutics in animal models of stroke, neurodegeneration, and cancer.
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| Enzyme Assay |
Not applicable. Non-cellular assays can assess TAT peptide binding to model membranes using SPR or liposome flotation assays. Biotinylated TAT peptide can be incubated with immobilized heparin or phospholipid vesicles. Binding is detected by streptavidin-HRP. Such assays confirm electrostatic interactions, but no traditional receptor binding IC50 is relevant.
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| Cell Assay |
Cellular uptake and delivery assay: Cells are seeded in 12-well plates. TAT peptide conjugated to a fluorescent protein or a fluorescent dye (0.1-10 uM) is added for 30-120 min. After washing, cells are trypsinized and analyzed by flow cytometry. For functional delivery, a TAT-Cre recombinase fusion protein is added to cells carrying a floxed reporter gene; Cre-mediated recombination is detected by a fluorescent reporter (e.g., GFP) or by PCR.
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| Animal Protocol |
Biodistribution and delivery model: Mice are injected intravenously with TAT peptide conjugated to a therapeutic protein (e.g., TAT-BDNF, 1-10 mg/kg). At 1-24 h post-injection, tissues are collected. Protein delivery is assessed by Western blot of tissue lysates, immunohistochemistry, or activity assays. For brain delivery, mice are perfused, and brain sections are stained for the delivered cargo. Behavior tests may be conducted for functional studies.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for TAT peptide alone are limited. As a 11-13 amino acid peptide (MW ~1600), it has a short plasma half-life (5-20 min in rodents) due to rapid proteolysis and renal excretion. It is water-soluble and typically administered intravenously or intraperitoneally. The peptide does not have significant oral bioavailability. Distribution includes kidney, liver, and brain.
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| Toxicity/Toxicokinetics |
Toxicity data for TAT peptide are limited. In vitro, it shows minimal cytotoxicity at concentrations ≤10 uM. In vivo, doses up to 10-20 mg/kg (i.p. or i.v.) are generally well tolerated in mice, with no significant acute toxicity. Higher doses may cause mild inflammatory responses. It is intended for research use only and not for human therapy. Standard precautions should be followed.
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| References |
[1]. Orzáez M, et al. Intrinsic caspase-8 activation mediates sensitization of erlotinib-resistant tumor cells toerlotinib/cell-cycle inhibitors combination treatment. Cell Death Dis. 2012 Oct 25;3:e415.
[2]. Lou L, et al. Functionalized magnetic-fluorescent hybrid nanoparticles for cell labelling. Nanoscale. 2011 May;3(5):2315-23. |
| Additional Infomation |
TAT peptide is a research-grade cell-penetrating peptide (CPP) widely used in molecular biology and drug delivery. It has not been approved for clinical use. The sequence is typically YGRKKRRQRRR (11-mer) or GRKKRRQRRRPPQ (13-mer). The TFA salt is used to improve solubility and stability. For research use only. Store at -20degC, desiccated and protected from light.
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| Molecular Formula |
C65H124N34O15
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| Related CAS # |
TAT peptide TFA
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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, 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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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