| Size | Price | Stock | Qty |
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| Targets |
HIV-1
HIV-1 TAT (48-60) targets the cell membrane and intracellular compartments, utilizing its cationic nature to interact with negatively charged cell surface components such as heparan sulfate proteoglycans. The peptide can translocate through the plasma membrane and reach the nucleus to transactivate the viral genome. It binds to the TAR RNA element and interacts with various transcriptional cofactors. As a cell-penetrating peptide, its primary target is the cellular membrane system, facilitating the delivery of exogenous molecules into the cytoplasm and nucleus via endocytotic and non-endocytotic mechanisms. |
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| ln Vitro |
Exogenous Tat protein can translocate across the plasma membrane and enter the nucleus, where it can activate the viral genome, according to studies. At the normal dosage of 1 mM, the HIV-1 TAT (48-60) peptide, which only comprises the basic domain of the full length peptide, maintains the entire translocation activity and even seems to be more effective in terms of nuclear localization when compared to the other active peptides[1]. Large, hydrophilic molecules can be delivered intracellularly using cell-penetrating peptides, which are thought to be a potential vector. Confocal laser scanning microscopy shows an apparent endocytotic absorption of HIV-1 TAT (48–60)[2]. The production of rod-shaped, possibly inverted micelles in DMPC is induced by HIV-1 TAT (48–60), and these micelles may serve as intermediates while translocating across eukaryotic membranes[3].
In vitro studies demonstrate that HIV-1 TAT (48-60) retains full translocation activity and appears more efficient in nuclear localization compared to other active peptides at standard doses of 1 mM. Confocal laser scanning microscopy reveals an apparently endocytotic uptake mechanism. The peptide induces the formation of rodlike, presumably inverted micelles in DMPC membranes, which may represent intermediates during translocation across eukaryotic membranes. These properties make it an effective vector for intracellular delivery of large, hydrophilic molecules in cell-based assays. |
| ln Vivo |
In vivo applications of HIV-1 TAT (48-60) focus on its ability to deliver therapeutic cargoes into tissues and organs. The peptide has been used in animal models to facilitate the delivery of proteins, peptides, and nucleic acids across biological barriers including the blood-brain barrier. Its membrane-penetrating properties allow for efficient biodistribution of conjugated molecules to various tissues following systemic administration. The peptide's in vivo efficacy is largely dependent on the cargo being delivered and the route of administration, with applications in cancer therapy, neurological disorders, and infectious disease research.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for HIV-1 TAT (48-60) typically involve assessing its interaction with cell surface receptors or model membranes. Surface plasmon resonance (SPR) can be used to measure binding affinity to heparan sulfate or other glycosaminoglycans. Fluorescence-based assays using labeled peptide variants allow for monitoring of membrane binding and translocation kinetics. The peptide is typically incubated with liposomes or isolated membrane fractions, and binding is quantified using fluorescence spectroscopy or radiolabeled tracer methods. Isothermal titration calorimetry (ITC) may also be employed to characterize thermodynamic parameters of binding.
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| Cell Assay |
Cellular assays for HIV-1 TAT (48-60) involve treating cultured cells with the peptide, either alone or conjugated to cargo molecules, to assess its cell-penetrating efficiency. Typical protocols use fluorescently labeled peptide (e.g., FITC-TAT) at concentrations ranging from 0.1-10 microM. Cells are incubated at 37degC for 1-24 hours, washed, and analyzed by flow cytometry or confocal microscopy to quantify uptake. Endocytosis inhibitors (e.g., chlorpromazine, dynasore, methyl-beta-cyclodextrin) are often used to elucidate the internalization mechanism. Cytotoxicity is assessed using MTT or LDH release assays.
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| Animal Protocol |
In vivo animal studies with HIV-1 TAT (48-60) typically involve administration of the peptide or its conjugates to rodent models via intravenous, intraperitoneal, or intranasal routes. For biodistribution studies, fluorescently or radioactively labeled peptide is administered, and tissue samples are collected at various time points post-injection for analysis. Organ distribution, plasma clearance, and tissue accumulation are quantified. In disease models, the peptide-conjugated therapeutic cargo is evaluated for efficacy, with appropriate control groups receiving unconjugated peptide or vehicle alone. Dosing regimens typically range from 0.1-10 mg/kg.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of HIV-1 TAT (48-60) are characterized by rapid distribution and clearance typical of small peptides. Following intravenous administration, the peptide has a short half-life due to rapid renal clearance and proteolytic degradation. The peptide is stable in powder form at -20degC for up to 3 years and in solution at -80degC for 6 months. Its small size (molecular weight ~1719 Da) and cationic nature facilitate rapid tissue distribution but also contribute to rapid elimination. Formulation strategies such as conjugation to larger carriers or PEGylation may be employed to prolong circulation time.
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| Toxicity/Toxicokinetics |
Toxicological assessment of HIV-1 TAT (48-60) indicates low cytotoxicity at concentrations typically used for cell penetration (1-10 microM). The peptide is not intended for therapeutic use and is supplied for research purposes only. At high concentrations, some cell lines may exhibit reduced viability due to membrane disruption. In animal studies, the peptide is generally well-tolerated at standard dosing ranges, though mild inflammatory responses may occur at administration sites. Standard toxicity endpoints include body weight monitoring, organ histopathology, and serum biochemistry in animal models.
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| References |
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| Additional Infomation |
HIV-1 TAT (48-60) is a widely used cell-penetrating peptide that serves as a model system for studying membrane translocation mechanisms and as a delivery vehicle for intracellular cargo delivery. It is not an approved therapeutic but is extensively used in research applications. The peptide sequence contains the basic domain (residues 49-57: RKKRRQRRR) responsible for its membrane-penetrating properties. Resistance to the peptide may involve mutations in the Tat transactivation domain that alter peptide-binding or transcriptional functions. Common combination strategies include co-administration with protease inhibitors or integrase inhibitors for enhanced antiviral activity in cell-based assays.
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| Molecular Formula |
C70H131N35O16
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| Molecular Weight |
1719.01
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| Exact Mass |
1720.066
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| CAS # |
220408-24-2
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| PubChem CID |
170907483
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| Appearance |
White to off-white solid powder
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| Density |
1.57±0.1 g/cm3(Predicted)
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| LogP |
-15.8
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| Hydrogen Bond Donor Count |
29
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| Hydrogen Bond Acceptor Count |
26
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| Rotatable Bond Count |
61
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| Heavy Atom Count |
121
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| Complexity |
3550
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| Defined Atom Stereocenter Count |
12
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| SMILES |
C(O)(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(N)=N)NC(=O)CN
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| InChi Key |
LEFRJAYXELYKGH-QDJQGUNISA-N
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| InChi Code |
InChI=1S/C70H133N35O16/c71-27-3-1-13-39(95-53(109)38(94-52(108)37-73)15-5-29-88-65(76)77)54(110)96-40(14-2-4-28-72)55(111)97-41(16-6-30-89-66(78)79)56(112)98-43(18-8-32-91-68(82)83)58(114)101-45(23-25-50(74)106)60(116)100-42(17-7-31-90-67(80)81)57(113)99-44(19-9-33-92-69(84)85)59(115)102-46(20-10-34-93-70(86)87)62(118)105-36-12-22-49(105)63(119)104-35-11-21-48(104)61(117)103-47(64(120)121)24-26-51(75)107/h38-49,51,107H,1-37,71-73,75H2,(H2,74,106)(H,94,108)(H,95,109)(H,96,110)(H,97,111)(H,98,112)(H,99,113)(H,100,116)(H,101,114)(H,102,115)(H,103,117)(H,120,121)(H4,76,77,88)(H4,78,79,89)(H4,80,81,90)(H4,82,83,91)(H4,84,85,92)(H4,86,87,93)/t38-,39-,40-,41-,42-,43-,44-,45-,46-,47-,48-,49-,51?/m0/s1
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| Chemical Name |
(2S)-5-amino-2-[[(2S)-1-[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-6-amino-2-[[(2S)-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)pentanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]-5-hydroxypentanoic 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 : ≥ 100 mg/mL (58.17 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (1.45 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 (1.45 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 (1.45 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 | 0.5817 mL | 2.9087 mL | 5.8173 mL | |
| 5 mM | 0.1163 mL | 0.5817 mL | 1.1635 mL | |
| 10 mM | 0.0582 mL | 0.2909 mL | 0.5817 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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