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| Targets |
FITC-LC-TAT (47-57) acetate targets the cell membrane and the intracellular environment. The TAT peptide is a classical CPP that is able to cross biological membranes, including the plasma membrane, via a non-receptor-mediated, endocytic process (primarily macropinocytosis). Its primary target is the entire cell interior. The FITC fluorophore is not a drug target but a tracer, enabling researchers to visualize and quantify the peptide's internalization. By labeling the TAT peptide with FITC, researchers can "target" specific cells for delivery of therapeutic molecules, but the probe itself serves only as a delivery and tracking tool. It has no specific protein receptor.
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| ln Vitro |
In vitro, the "activity" of FITC-LC-TAT (47-57) acetate is its ability to efficiently enter cells in a concentration- and time-dependent manner. It is an assay tool, not a therapeutic. When added to cell culture media (1-10 uM), it rapidly internalizes into various cell lines (HeLa, CHO, Jurkat) within 15-60 minutes. Internalization can be visualized by green fluorescence using a FITC filter (Ex/Em 490/525 nm). This activity can be blocked by chilling the cells (4degC) or treating them with endocytosis inhibitors (e.g., dynasore, chlorpromazine), confirming an energy-dependent uptake pathway. It is used to validate the cell-penetrating capacity of TAT in a specific model system before conjugating it to a therapeutic cargo.
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| ln Vivo |
In vivo, FITC-LC-TAT (47-57) acetate is used for optical imaging and biodistribution studies in small animals. Upon intravenous (IV) injection into mice (e.g., 1-5 mg/kg), the peptide rapidly distributes to major organs, particularly the kidneys and liver, due to its high hydrophilicity and rapid renal clearance. The FITC fluorescence can be detected using an in vivo imaging system (IVIS) within 30 minutes post-injection. This is used to assess the pharmacokinetics and biodistribution of the TAT peptide vector, providing a baseline for how conjugated drugs might behave. However, rapid clearance is a common challenge for CPP-based delivery in vivo.
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| Enzyme Assay |
General protocol for in vitro enzyme/receptor binding (non-cellular): Not applicable. FITC-LC-TAT (47-57) acetate does not specifically bind to an enzyme or receptor in a cell-free system. For a binding assay, the protocol is trivial: dissolve the peptide in PBS or water. Its chemical properties are stability and aqueous solubility. It can be analyzed by HPLC (C18 column, 0.1% TFA in water/acetonitrile gradient) to confirm purity, which is typically >95%.
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| Cell Assay |
General protocol for in vitro cell-based experiments: Culture HeLa cells in DMEM + 10% FBS to 80% confluency in a 96-well plate. Dilute FITC-LC-TAT (47-57) acetate in serum-free media to final concentrations of 1, 5, and 10 uM. Add the diluted peptide to the cells. Incubate at 37degC for 30-60 minutes. Aspirate the media and wash the cells 3x with PBS to remove extracellular peptide. Visualize under a fluorescent microscope (FITC filter) or detach cells with trypsin and analyze by flow cytometry (FL-1 channel, 515-545 nm). For a quantitative uptake assay, treat cells with 10 uM peptide, wash, lyse cells with 0.1% Triton X-100, and measure fluorescence intensity using a plate reader (Ex/Em 490/520 nm). Store peptide in the dark at -80degC.
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| Animal Protocol |
General protocol for in vivo animal experiments: For an imaging study, use 6-8 week old female BALB/c nude mice (20-25 g). Prepare a 2 mg/mL solution of FITC-LC-TAT (47-57) acetate in sterile PBS (pH 7.4). Inject 100 uL (200 ug, approx. 8 mg/kg) into the tail vein. At time points 30 min, 1 h, 2 h, and 4 h post-injection, euthanize the mice. Harvest major organs (liver, kidney, spleen, heart, lung, brain). Image the organs using an IVIS spectrum or similar system (Ex/Em 480/520 nm). Alternatively, homogenize the organs, extract the fluorescence in PBS, and quantify using a fluorescence plate reader to determine the percentage of injected dose per gram of tissue (%ID/g). The kidneys typically show the highest accumulation.
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| ADME/Pharmacokinetics |
General pharmacokinetic properties: FITC-LC-TAT (47-57) acetate has a molecular weight of 2061.38 g/mol (free base). It is a highly soluble peptide (>100 mg/mL in water). In vivo, it exhibits rapid clearance (t1/2 alpha < 5 minutes) due to renal filtration and proteolytic degradation. It is not orally bioavailable. It is not metabolized by CYP450 enzymes. After IV administration in mice, the peptide is detectable in plasma for less than 30 minutes. Its large molecular size prevents easy diffusion across the BBB. It is best stored as a powder at -20degC for up to 3 years.
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| Toxicity/Toxicokinetics |
General toxicity profile: FITC-LC-TAT (47-57) acetate is generally considered non-toxic at the low concentrations used for staining (1-10 uM) in vitro. In vivo, at the standard imaging dose (~8 mg/kg), it is well-tolerated in mice with no reports of acute toxicity, weight loss, or adverse behavioral changes. However, as a cationic peptide, very high doses may cause some non-specific membrane disruption. The FITC fluorophore is standard and has a well-established low toxicity profile for research use. Standard laboratory safety (gloves, lab coat) is sufficient. It is for research use only.
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| References |
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| Additional Infomation |
The TAT peptide sequence (47-57) is YGRKKRRQRRR. This is one of the most widely studied and utilized CPPs. The inclusion of the "LC" (aminohexanoic acid) spacer provides a flexible linker between the FITC and the peptide, reducing potential steric hindrance and improving labeling efficiency. The acetate salt form improves solubility and handling. This product is strictly for research purposes, not for human diagnostic or therapeutic use. It is a powerful tool for studying endocytosis, drug delivery, and intracellular targeting.
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| Molecular Formula |
C91H141N35O19S.XC2H4O2
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| Molecular Weight |
2061.38 (free base)
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| Related CAS # |
FITC-LC-TAT (47-57)
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| Sequence |
FITC-LC-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-NH2FITC-LC-YGRKKRRQRRR-NH2
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| Appearance |
Yellow to orange 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) |
H2O : ≥ 100 mg/mL
DMSO : ~3.57 mg/mL (with sonication) |
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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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