![Cys-TAT(47-57) TFA (Cys-[HIV-Tat (47-57)] TFA)](/upload/1124/V77112.png)
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| Targets |
Cys-TAT(47-57) TFA does not target a specific cell surface receptor; its mechanism of action is based on direct transduction across the plasma membrane. The TAT domain (47-57, sequence YGRKKRRQRRR) contains multiple arginine residues whose positive charges interact electrostatically with negatively charged membrane phospholipids and heparan sulfate proteoglycans, initiating cellular internalization primarily via macropinocytosis and direct translocation.
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| ln Vitro |
The in vitro activity of Cys-TAT(47-57) is assessed by its ability to deliver conjugated cargo (e.g., fluorescent dyes, peptides, proteins, siRNA) into various cell lines. As a delivery vehicle, it has no intrinsic inhibitory or stimulatory activity on its own. The uptake efficiency is concentration-dependent, typically optimal at 1-10 microM. The peptide can facilitate the intracellular delivery of otherwise impermeable compounds in a non-toxic manner. Cys-TAT(47-57) also binds electrostatically to plasmid DNA for gene delivery applications.
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| ln Vivo |
The most relevant in vivo activity is the facilitation of intracellular drug delivery following systemic or local administration of TAT-conjugated therapeutics. The unmodified TAT peptide itself can induce some systemic distribution of conjugated molecules, including crossing of the blood-brain barrier (BBB) to a limited extent. The major therapeutic application of TAT-based delivery is in oncology and neurology, where it enhances tumor penetration and neuronal uptake. Direct toxicity of the carrier peptide is minimal at standard delivery doses.
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| Enzyme Assay |
The ability of Cys-TAT(47-57) to translocate across membranes is assessed in acellular model systems using large unilamellar vesicles (LUVs) composed of synthetic phospholipids. The peptide is incubated with lipid vesicles containing a fluorescent dye (e.g., calcein). Membrane translocation is detected by monitoring dye leakage or by measuring peptide-induced fluorescence anisotropy changes of membrane-embedded probes. Circular dichroism (CD) spectroscopy is used to study conformational changes of the peptide in the presence of lipid vesicles or membrane-mimetic environments.
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| Cell Assay |
Cellular uptake of Cys-TAT(47-57) is quantified by flow cytometry and confocal microscopy. Cells (e.g., HeLa, HEK-293, CHO-K1) are seeded in 24-well plates (1-2 × 10⁵ cells/well) and grown overnight. The cells are then incubated with various concentrations (0.1-20 microM) of fluorescently labeled Cys-TAT(47-57) (e.g., tagged with FITC, Cy5, or TAMRA) in serum-free or serum-containing media for 1-4 hours at 37degC. After extensive washing to remove surface-bound peptide, cells are trypsinized and analyzed by flow cytometry (excitation/emission matched to the fluorophore). Confocal microscopy images confirm intracellular localization. To assess internalization mechanisms, cells are pre-incubated with inhibitors (e.g., chlorpromazine for clathrin, genistein for caveolae, cytochalasin D for macropinocytosis, or low temperature (4degC) to block energy-dependent endocytosis) before adding the fluorescent peptide.
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| Animal Protocol |
Cys-TAT(47-57) itself is not an active pharmaceutical ingredient. However, in animal studies, TAT-conjugated therapeutic cargos are administered intravenously (i.v.), intraperitoneally (i.p.), or intratumorally. A typical protocol to assess delivery efficiency: fluorescently labeled Cys-TAT(47-57) conjugate (e.g., TAT-Cy5.5) is administered to mice at a dose of 1-10 mg/kg via tail vein injection. At predetermined time points (e.g., 1, 4, 8, 24 hours), mice are sacrificed and major organs (liver, kidney, spleen, lung, heart, brain) are harvested. Organs are imaged using an in vivo imaging system (IVIS) to assess biodistribution. Alternatively, tissue sections are examined by fluorescence microscopy for cellular localization.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of Cys-TAT(47-57) are based on the Tat (47-57) sequence. The arginine-rich CPP is generally unstable in blood circulation due to rapid proteolytic degradation and kidney filtration. The plasma half-life is typically less than 30-60 minutes in rodents. It accumulates primarily in the kidneys and liver after systemic administration, with rapid renal clearance as the major elimination pathway. Formulation in PEGylated liposomes or conjugation to larger macromolecules significantly improves its plasma stability and circulation time.
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| Toxicity/Toxicokinetics |
Toxicity assessments of Cys-TAT(47-57) in vitro indicate low cytotoxicity up to concentrations of 30-50 microM in various cell types (HeLa, HEK-293, primary neurons). At very high concentrations (≥100 microM), membrane disruption and signs of cytolysis may occur due to excessive positive charge. In animal models, systemic administration of up to 10 mg/kg does not result in significant acute toxicity, weight loss, or histopathological changes in major organs. Hemolysis is a potential concentration-dependent concern that must be monitored for i.v. formulations.
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| References | |
| Additional Infomation |
Cys-TAT(47-57) is the TFA salt of the cell-penetrating peptide (CPP) derived from HIV-1 Tat protein residues 47-57 (YGRKKRRQRRR). The C-terminal cysteine allows maleimide- or iodoacetamide-based covalent conjugation to thiol-reactive groups on payload molecules, while the TFA counterion improves handling and solubility. TAT-mediated delivery has revolutionized intracellular targeting of large polar molecules that otherwise cannot cross the lipid bilayer. This product is strictly for research use; no clinical formulations are approved based solely on the CPP conjugate alone.
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| Molecular Formula |
C69H125F3N34O16S
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| Molecular Weight |
1776.01
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| Related CAS # |
Cys-TAT(47-57);583836-55-9
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| Appearance |
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) |
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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.5631 mL | 2.8153 mL | 5.6306 mL | |
| 5 mM | 0.1126 mL | 0.5631 mL | 1.1261 mL | |
| 10 mM | 0.0563 mL | 0.2815 mL | 0.5631 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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