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TAT peptide TFA

Cat No.:V76453 Purity: ≥98%
TAT peptide (TFA) is a cell-penetrating/penetrable peptide (GRKKRRQRRRPQ) developed from HIV-1 reverse transcription activator (Tat).
TAT peptide TFA
TAT peptide TFA Chemical Structure Product category: HIV
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

Other Forms of TAT peptide TFA:

  • sgp91 ds-tat Peptide 2, scrambled
  • TAT peptide
Official Supplier of:
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Top Publications Citing lnvivochem Products
Product Description
TAT peptide (TFA) is a cell-penetrating/penetrable peptide (GRKKRRQRRRPQ) developed from HIV-1 reverse transcription activator (Tat).
TAT peptide TFA is a cell-penetrating peptide derived from the transactivator of transcription (Tat) protein of HIV-1. It corresponds to the basic domain (residues 47-57, sequence YGRKKRRQRRR) and is widely used to deliver a variety of macromolecular cargos, including proteins, peptides, nucleic acids, and nanoparticles, into living cells. The TFA salt enhances solubility and stability.
Biological Activity I Assay Protocols (From Reference)
Targets
HIV-1
No specific biological target. The TAT peptide functions as a cell-penetrating peptide (CPP) that mediates the delivery of conjugated cargo across the plasma membrane via a non-toxic, energy-dependent or independent mechanism. It interacts with cell surface heparan sulfate proteoglycans and other membrane components to facilitate cellular uptake.
ln Vitro
The trans-activating transcriptional activator (Tat) from HIV-1 is the source of the cell penetrating peptide known as TAT peptide (TFA) (GRKKRRQRRRPQ)[1]. Because TAT peptide (TFA)(GRKKRRQRRRPQ) functionalized hybrid nanoparticles combine optical detection and magnetic enrichment for quick and easy cell labeling, they are also being explored. An
TAT peptide TFA efficiently translocates across cell membranes and delivers conjugated cargoes into the cytoplasm and nucleus of a wide range of cell types. In vitro, it is used to study intracellular protein function, deliver therapeutic molecules, and evaluate endocytic pathways. The peptide retains its transduction activity after covalent attachment to cargo.
ln Vivo
In vivo, TAT peptide TFA has been used to deliver various bioactive cargos, including peptides, proteins, and nucleic acids, to tissues such as the brain, heart, and tumors. Systemic administration leads to broad biodistribution. It serves as a research tool for studying the therapeutic potential of intracellular protein delivery and for targeting diseases where cytosolic access is required.
Enzyme Assay
Not applicable. TAT peptide is not a receptor ligand. However, surface plasmon resonance (SPR) can be used to study its interaction with model membranes or heparin. Biotinylated TAT peptide can be immobilized on a sensor chip, and increasing concentrations of heparin or other binding partners can be injected. Binding affinity is calculated from association/dissociation rates.
Cell Assay
Cellular uptake assay: Cells are seeded in 96-well plates (1×10⁴ cells/well). Fluorescently labeled TAT peptide TFA (0.1-10 uM) is added to the culture medium and incubated for 30-120 min at 37degC. Cells are washed, fixed, and counterstained with DAPI and membrane dye. Uptake is quantified by fluorescence microscopy, flow cytometry, or a plate reader after lysing the cells. Endocytic inhibitors (e.g., cytochalasin D) can be used to study uptake mechanism.
Animal Protocol
In vivo biodistribution model: Mice are injected intravenously or intraperitoneally with fluorescently labeled TAT peptide TFA (1-10 mg/kg). At various time points (0.5-24 h), organs (liver, kidney, brain, heart, lung) are harvested, sectioned, and imaged by fluorescence microscopy. Alternatively, radiolabeled TAT peptide is used, and organ radioactivity is counted. The peptide is used to study tissue penetration and delivery efficiency.
ADME/Pharmacokinetics
As a synthetic peptide (MW 1563.88, TFA salt), TAT peptide has a short plasma half-life (minutes) due to rapid proteolytic degradation and renal clearance. It is typically administered via intravenous, intraperitoneal, or intrathecal injection for in vivo studies. The peptide is water-soluble and stable when stored as a lyophilized powder at -20degC.
Toxicity/Toxicokinetics
Toxicity data for TAT peptide TFA are limited. At standard concentrations (1-10 uM in vitro; 1-10 mg/kg in mice), it is generally non-cytotoxic and well-tolerated. High doses may cause non-specific membrane disruption or immune activation. The peptide is intended for research use only and not for human therapeutic applications. Standard safety precautions for handling peptides should be observed.
References

[1]. 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]. Functionalized magnetic-fluorescent hybrid nanoparticles for cell labelling. Nanoscale. 2011 May;3(5):2315-23.

Additional Infomation
TAT peptide TFA is a research-grade cell-penetrating peptide derived from HIV-1 Tat. It has not entered clinical trials or received regulatory approval for human therapeutic use. It is a widely used tool in drug delivery, molecular imaging, and intracellular targeting. The sequence is YGRKKRRQRRR-NH2 or YGRKKRRQRRR (commonly). For research use only. Store at -20degC, protected from light and moisture.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C67H125F3N34O17
Molecular Weight
1735.93
Related CAS #
TAT peptide
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)
H2O :≥ 50 mg/mL (~28.80 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.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 0.5761 mL 2.8803 mL 5.7606 mL
5 mM 0.1152 mL 0.5761 mL 1.1521 mL
10 mM 0.0576 mL 0.2880 mL 0.5761 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.

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An example of molarity calculation using the molarity calculator is shown below:
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?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
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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:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
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  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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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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