| Size | Price | Stock | Qty |
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| Targets |
The primary "target" of TAT 48-57 is not a specific protein receptor but rather the cell membrane itself. As a cell-penetrating peptide, it facilitates the translocation of cargo across the lipid bilayer of cell membranes through non-receptor-dependent mechanisms. The peptide interacts with the cell membrane via electrostatic interactions between its positively charged arginine residues and negatively charged components of the membrane, such as heparan sulfate proteoglycans. Following membrane interaction, the peptide and its cargo are internalized through various endocytic pathways, including macropinocytosis and clathrin-mediated endocytosis. Once inside the cell, TAT 48-57 can interact with intracellular targets to enhance the transcriptional activity of HIV-1.
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| ln Vitro |
TAT (48-57) is a short, cell-permeable peptide that is good at passing the cell membranes of diverse cell types. It has low overall toxicity and will not leak out of the cells after internalization [1].
TAT 48-57 is a short, cell-permeable peptide that is highly efficient at crossing the cell membranes of diverse cell types. In vitro studies have demonstrated that the peptide has low overall toxicity and does not leak out of cells after internalization. Its cell-penetrating activity has been extensively characterized in various cell lines, showing that the peptide can efficiently deliver cargo molecules into the cytoplasm and nucleus. The peptide's ability to cross membranes is attributed to its arginine-rich sequence, which facilitates electrostatic interactions with the cell surface. TAT 48-57 is also used to study viral gene expression and replication by interacting with intracellular targets to enhance the transcriptional activity of HIV-1. |
| ln Vivo |
In vivo, TAT 48-57 is used as a delivery vehicle to transport therapeutic molecules across biological barriers, including the blood-brain barrier. The peptide has been shown to facilitate the delivery of various cargoes, such as proteins, peptides, and nucleic acids, to tissues and organs in animal models. Its ability to cross cell membranes and reach intracellular targets makes it a valuable tool for in vivo drug delivery studies. The peptide's low toxicity and lack of leakage from cells after internalization make it suitable for in vivo applications. It has been used in preclinical studies for the delivery of neuroprotective agents, anticancer drugs, and gene therapy vectors.
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| Enzyme Assay |
Cell-free enzyme/receptor binding assays are not typically performed for TAT 48-57, as its mechanism does not involve binding to a specific enzyme or receptor. However, its membrane-interacting properties can be studied using model membrane systems such as liposomes. A typical protocol involves preparing liposomes of defined lipid composition and incubating them with fluorescently labeled TAT 48-57. The binding and insertion of the peptide into the lipid bilayer can be monitored by fluorescence spectroscopy or by measuring changes in membrane permeability. Alternatively, surface plasmon resonance (SPR) can be used to study the interaction of TAT 48-57 with immobilized lipid bilayers or heparan sulfate. These assays provide insights into the molecular basis of the peptide's cell-penetrating activity.
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| Cell Assay |
For in vitro cellular experiments, cells are cultured in appropriate media and treated with TAT 48-57 at concentrations ranging from 1-50 microM. The peptide can be used alone or as a carrier for various cargoes. To study cellular uptake, fluorescently labeled TAT 48-57 is added to the culture medium, and cells are incubated for 1-4 hours at 37degC. After incubation, cells are washed thoroughly to remove extracellular peptide and analyzed by fluorescence microscopy or flow cytometry. For cargo delivery studies, the cargo is conjugated to TAT 48-57, and the uptake and intracellular distribution of the cargo are assessed. The duration of treatment and concentration of the peptide can be optimized depending on the cell type and the specific experimental objectives.
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| Animal Protocol |
In vivo animal experiments with TAT 48-57 typically involve intravenous or intraperitoneal administration of the peptide or its conjugates in mice or rats. A common dosing regimen is 1-10 mg/kg body weight. The peptide is administered to study its biodistribution, tissue penetration, and ability to deliver cargo to target organs. For studies involving the delivery of therapeutic agents, the peptide-cargo conjugate is administered, and therapeutic efficacy is assessed by measuring disease progression, tumor growth, or other relevant endpoints. The peptide's ability to cross the blood-brain barrier is evaluated by measuring the concentration of the peptide or its cargo in brain tissue. Blood and tissue samples are collected for pharmacokinetic and biodistribution analysis.
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| ADME/Pharmacokinetics |
TAT 48-57 is a peptide with a molecular weight of approximately 1,257.5 g/mol. It is typically provided as a lyophilized powder and should be stored at -20degC. The peptide is soluble in water and aqueous buffers. As a cell-penetrating peptide, its pharmacokinetic properties are characterized by rapid clearance from the circulation and extensive tissue distribution. The peptide is subject to proteolytic degradation in vivo, which limits its half-life. Its bioavailability and half-life can be improved through chemical modifications, such as cyclization or the incorporation of D-amino acids. The peptide is for research use only and is not approved for clinical use.
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| Toxicity/Toxicokinetics |
TAT 48-57 is generally considered to have low toxicity. In vitro studies have shown that the peptide is well-tolerated by various cell types at concentrations up to 50 microM, with no significant effects on cell viability or proliferation. In vivo, the peptide has been shown to be safe at therapeutic doses, with no significant adverse effects reported in animal studies. However, as with any peptide, high doses may cause immune responses or other adverse effects. The peptide should be handled with care to avoid inhalation, contact with eyes and skin, and the formation of dust or aerosols. Use only in areas with appropriate exhaust ventilation. The compound is for research use only and not for human therapeutic use.
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| References | |
| Additional Infomation |
TAT 48-57 is a classical cell-penetrating peptide derived from the HIV-1 Tat protein. Its sequence consists of amino acid residues 48 to 57 of the Tat protein: Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg. The peptide is rich in arginine residues, which confer its cell-penetrating properties through electrostatic interactions with the cell membrane. TAT 48-57 is widely used as a tool for intracellular delivery of various macromolecules, including proteins, peptides, nucleic acids, and nanoparticles. It has been extensively studied for its potential applications in drug delivery, gene therapy, and the treatment of various diseases. The peptide is available as a research compound and is not approved for clinical use. Its ability to efficiently deliver cargo into cells makes it a valuable tool in biomedical research.
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| Molecular Formula |
C55H109N31O12
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| Molecular Weight |
1396.65446639061
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| Exact Mass |
1395.887
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| CAS # |
253141-50-3
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| Related CAS # |
TAT (48-57) (TFA)
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| PubChem CID |
78298635
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| Appearance |
White to off-white solid powder
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| LogP |
-14.5
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| Hydrogen Bond Donor Count |
26
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| Hydrogen Bond Acceptor Count |
21
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| Rotatable Bond Count |
54
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| Heavy Atom Count |
98
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| Complexity |
2710
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(C(CCCCN)NC(C(CCCCN)NC(C(CCC/N=C(\N)/N)NC(CN)=O)=O)=O)NC(C(NC(C(NC(C(NC(C(NC(C(NC(C(=O)O)CCC/N=C(\N)/N)=O)CCC/N=C(\N)/N)=O)CCC/N=C(\N)/N)=O)CCC(N)=O)=O)CCC/N=C(\N)/N)=O)CCC/N=C(\N)/N
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| InChi Key |
AJFGTSYBZVRLJD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C55H109N31O12/c56-21-3-1-11-31(79-41(89)30(78-40(88)29-58)13-5-23-72-50(60)61)42(90)80-32(12-2-4-22-57)43(91)81-33(14-6-24-73-51(62)63)44(92)82-35(16-8-26-75-53(66)67)46(94)85-37(19-20-39(59)87)48(96)84-34(15-7-25-74-52(64)65)45(93)83-36(17-9-27-76-54(68)69)47(95)86-38(49(97)98)18-10-28-77-55(70)71/h30-38H,1-29,56-58H2,(H2,59,87)(H,78,88)(H,79,89)(H,80,90)(H,81,91)(H,82,92)(H,83,93)(H,84,96)(H,85,94)(H,86,95)(H,97,98)(H4,60,61,72)(H4,62,63,73)(H4,64,65,74)(H4,66,67,75)(H4,68,69,76)(H4,70,71,77)
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| Chemical Name |
2-[[2-[[2-[[5-amino-2-[[2-[[2-[[6-amino-2-[[6-amino-2-[[2-[(2-aminoacetyl)amino]-5-(diaminomethylideneamino)pentanoyl]amino]hexanoyl]amino]hexanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-5-oxopentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoic acid
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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) |
DMSO : ~50 mg/mL (~35.80 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (1.79 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (1.79 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (1.79 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.7160 mL | 3.5800 mL | 7.1600 mL | |
| 5 mM | 0.1432 mL | 0.7160 mL | 1.4320 mL | |
| 10 mM | 0.0716 mL | 0.3580 mL | 0.7160 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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