| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
TAT-amide does not target a specific receptor or enzyme; rather, it interacts with cell surface heparan sulfate proteoglycans and lipid bilayers to initiate non-receptor-mediated endocytosis (macropinocytosis and clathrin-mediated pathways) and possibly direct membrane translocation at higher concentrations. Its primary function is as a delivery vehicle, not a pharmacological modulator of a specific protein.
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| ln Vitro |
For the cellular delivery of cargos like DNA, siRNA, organic halides, ruthenium complexes, Zr-labeled antibodies for PET imaging, low molecular weight chitosan, and fluorescent dyes, cell-penetrating peptides (CPPs) have been employed [2].
In vitro, TAT-amide demonstrates high efficiency in delivering a wide range of cargoes (e.g., DNA plasmids, siRNA, proteins, peptides, quantum dots, liposomes, and small molecules) into multiple cell lines, including HeLa, CHO, Jurkat, and primary neurons. At concentrations of 1-10 uM, it penetrates >90% of cells within 1 hour with no significant cytotoxicity. The uptake is energy-dependent at 37degC but also shows some energy-independent mechanisms at 4degC. It can co-localize in the cytosol and nucleus (due to its nuclear localization signal-like sequence). |
| ln Vivo |
In vivo, TAT-amide has been used to deliver therapeutic peptides and antisense oligonucleotides across the blood-brain barrier. For example, intraperitoneal or intravenous injection of TAT-amide fused to Bcl-xL (an anti-apoptotic protein) reduces infarct volume in a mouse model of focal cerebral ischemia. Similarly, TAT-amide conjugated to a peptide inhibitor of JNK (D-JNKI1) provides neuroprotection in models of stroke and spinal cord injury. The peptide itself (without cargo) has no intrinsic biological effect other than potential immunogenicity or mild cellular stress.
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| Enzyme Assay |
Standard cell-free assays are not applicable for a cell-penetrating peptide, as its function relies on membrane interaction. However, artificial membrane models such as large unilamellar vesicles (LUVs) composed of phosphatidylcholine/phosphatidylglycerol (80:20) can be used. TAT-amide (0.1-10 uM) is incubated with LUVs containing encapsulated fluorescent dye (calcein). Membrane permeabilization is measured by fluorescence dequenching (ex 485 nm, em 535 nm). Alternatively, surface plasmon resonance (SPR) can assess binding affinity to immobilized heparin or lipid bilayers.
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| Cell Assay |
HeLa or CHO cells are seeded in 8-well chamber slides or 96-well plates at 50% confluency. Cells are incubated with fluorescein-labeled TAT-amide (5-50 uM) in serum-free medium for 15-60 minutes at 37degC. After washing with heparin-containing buffer (to remove surface-bound peptide), cells are fixed with 4% paraformaldehyde, and uptake is visualized by confocal microscopy or quantified by flow cytometry (ex 488 nm, em 525 nm). To distinguish endocytosis from direct penetration, cells are pre-treated with endocytosis inhibitors (chlorpromazine, genistein, or wortmannin) or incubated at 4degC.
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| Animal Protocol |
Male BALB/c mice (20-25 g) receive a single intravenous injection of fluorescein-labeled TAT-amide (5-10 mg/kg) or TAT-amide conjugated to a therapeutic cargo. At various time points (15 min, 1 h, 4 h, 24 h), animals are perfused with PBS, and tissues (brain, liver, kidney, heart, lung) are harvested. Frozen sections are examined by fluorescence microscopy for tissue distribution. For efficacy studies, disease models (e.g., stroke or tumor xenograft) are treated with TAT-cargo conjugates at doses of 1-20 mg/kg (i.v. or i.p.) daily for 3-7 days, and outcomes (infarct size, tumor volume) are measured.
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| ADME/Pharmacokinetics |
As a peptide, TAT-amide has a short plasma half-life (t½ ≈ 5-15 minutes in mice) due to rapid renal clearance and proteolytic degradation. The amidated C-terminus increases resistance to carboxypeptidases, but it is still susceptible to endopeptidases. Peak plasma concentration is reached immediately after bolus injection. The peptide distributes widely, with high accumulation in kidney and liver; brain concentrations are approximately 1-5% of plasma levels. Co-administration with protease inhibitors or formulation in nanoparticles can prolong exposure.
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| Toxicity/Toxicokinetics |
TAT-amide is generally considered non-toxic at concentrations up to 10 uM in cell culture and up to 20 mg/kg in mice. At higher doses (>50 mg/kg i.v.), it can cause mild hemolysis and transient hypotension due to non-specific membrane disruption. Repeated administration may elicit anti-TAT antibody production, leading to reduced efficacy and potential immune complex deposition. No genotoxicity or cardiotoxicity has been reported. The peptide is not cytotoxic to primary neurons at 10 uM for 24 hours.
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| References |
[1]. Xu P, et al. Precise control of apoptosis via gold nanostars for dose dependent photothermal therapy of melanoma. J Mater Chem B. 2019 Nov 28;7(44):6934-6944.
[2]. Okuda-Shinagawa NM, et al. Fluorescent and Photosensitizing Conjugates of Cell-Penetrating Peptide TAT(47-57): Design, Microwave-Assisted Synthesis at 60 °C, and Properties. ACS Omega. 2017 Nov 30;2(11):8156-8166. |
| Additional Infomation |
This peptide is exclusively a research tool for drug delivery, intracellular imaging, and gene therapy studies. It is not approved for human use by any regulatory agency, and no clinical trials have been conducted with TAT-amide alone (although TAT-fusion proteins have entered early-phase trials). The compound is often used as a positive control in CPP studies. Deuterated and biotinylated versions are available for PK and interaction studies. It should be stored as a lyophilized powder at -20degC.
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| Molecular Formula |
C64H119N33O13
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| Molecular Weight |
1558.8430
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| Exact Mass |
1557.966
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| CAS # |
697226-52-1
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| Related CAS # |
TAT-amide TFA
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| PubChem CID |
101905519
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
-11.9
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| Hydrogen Bond Donor Count |
28
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| Hydrogen Bond Acceptor Count |
22
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| Rotatable Bond Count |
58
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| Heavy Atom Count |
110
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| Complexity |
3090
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| Defined Atom Stereocenter Count |
10
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| SMILES |
C1=CC(=CC=C1C[C@@H](C(=O)NCC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N)N)O
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| InChi Key |
FHNRCIMBMGTCBF-AGVBWZICSA-N
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| InChi Code |
InChI=1S/C64H119N33O13/c65-25-3-1-11-40(91-51(103)39(14-6-28-83-60(72)73)89-48(100)34-88-50(102)37(67)33-35-19-21-36(98)22-20-35)53(105)92-41(12-2-4-26-66)54(106)94-43(16-8-30-85-62(76)77)55(107)95-45(18-10-32-87-64(80)81)57(109)97-46(23-24-47(68)99)58(110)96-44(17-9-31-86-63(78)79)56(108)93-42(15-7-29-84-61(74)75)52(104)90-38(49(69)101)13-5-27-82-59(70)71/h19-22,37-46,98H,1-18,23-34,65-67H2,(H2,68,99)(H2,69,101)(H,88,102)(H,89,100)(H,90,104)(H,91,103)(H,92,105)(H,93,108)(H,94,106)(H,95,107)(H,96,110)(H,97,109)(H4,70,71,82)(H4,72,73,83)(H4,74,75,84)(H4,76,77,85)(H4,78,79,86)(H4,80,81,87)/t37-,38-,39-,40-,41-,42-,43-,44-,45-,46-/m0/s1
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| Chemical Name |
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[2-[[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]acetyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]hexanoyl]amino]hexanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-N-[(2S)-1-[[(2S)-1-[[(2S)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]pentanediamide
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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) |
H2O : ≥ 65 mg/mL (~41.70 mM)
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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 | 0.6415 mL | 3.2075 mL | 6.4150 mL | |
| 5 mM | 0.1283 mL | 0.6415 mL | 1.2830 mL | |
| 10 mM | 0.0642 mL | 0.3208 mL | 0.6415 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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