| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
TAT-14 targets the Keap1 protein by binding to the Nrf2 binding site on Keap1. This competitive disruption of the Nrf2-Keap1 interaction stabilizes cytosolic Nrf2, promoting its nuclear translocation and binding to the antioxidant response element (ARE).
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|---|---|
| ln Vitro |
In vitro, TAT-14 increases Nrf2 protein levels in a dose-dependent manner without affecting Nrf2 mRNA expression. In human THP-1 monocyte cells, it significantly activates the expression of heme oxygenase-1 (HO-1), an anti-inflammatory gene downstream of Nrf2, at concentrations as low as 37.5 μM. It also inhibits the production of the pro-inflammatory cytokine TNF.
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| ln Vivo |
In vivo, TAT-14 exhibits anti-inflammatory properties by activating the Nrf2 pathway. While specific in vivo animal model data for this peptide is limited in the provided sources, its mechanism of action as a cell-penetrating peptide targeting the Nrf2/Keap1 interaction suggests potential therapeutic applications in inflammatory conditions.
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| Enzyme Assay |
Non-cellular assays for TAT-14 typically involve studying its direct interaction with the Keap1 protein. This can be assessed using techniques such as surface plasmon resonance (SPR) or isothermal titration calorimetry (ITC) to measure the binding affinity between TAT-14 and recombinant Keap1, confirming its ability to competitively inhibit the Nrf2-Keap1 interaction.
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| Cell Assay |
In vitro cellular assays are performed by treating cells, such as human THP-1 monocytes, with TAT-14. Following treatment, the levels of Nrf2 protein are measured via Western blot, showing a peak at 3 hours. The activation of downstream target genes, like HO-1, is assessed by measuring HO-1 mRNA (peaking at 6 hours) and protein levels (peaking at 12 hours) using qRT-PCR and Western blot, respectively. The anti-inflammatory effect is confirmed by measuring the inhibition of TNF production.
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| Animal Protocol |
In vivo animal experiments for TAT-14 would likely involve administering the peptide to animal models of inflammation, such as mice with induced inflammatory conditions. The efficacy would be evaluated by measuring inflammatory markers, assessing tissue damage, and monitoring clinical signs of inflammation, although specific protocols are not detailed in the provided references.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties: Specific PK data for TAT-14 is not provided in the available sources. As a peptide, its properties would be influenced by factors such as sequence, stability, and formulation. Its design as a cell-penetrating peptide suggests an ability to cross biological membranes, which is crucial for its intracellular target, Keap1.
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| Toxicity/Toxicokinetics |
Toxicological profile: Specific toxicological data for TAT-14 is not available in the provided sources. As a research compound, its safety profile would be determined through standard preclinical toxicology studies. It is intended for research use only and not for human consumption.
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| References | |
| Additional Infomation |
Other information: TAT-14 has a molecular weight of 3173.59 for the free base and 3287.61 for the TFA salt form, with a CAS number of 1362661-34-4. It is soluble in water and should be stored as a powder at -20°C for long-term stability. It serves as a valuable chemical biology tool for studying the Nrf2 pathway and has potential therapeutic applications in inflammation and other diseases where Nrf2 plays a protective role.
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| Molecular Formula |
C8H5D3O2
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|---|---|
| Molecular Weight |
139.17
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| Exact Mass |
139.071
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| CAS # |
342611-04-5
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| Related CAS # |
4-Methoxybenzaldehyde;123-11-5
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| PubChem CID |
57894594
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
248.0±0.0 °C at 760 mmHg
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| Flash Point |
108.9±0.0 °C
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| Vapour Pressure |
0.0±0.5 mmHg at 25°C
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| Index of Refraction |
1.547
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| LogP |
1.7
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
10
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| Complexity |
104
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| Defined Atom Stereocenter Count |
0
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| SMILES |
[2H]C([2H])([2H])OC1=CC=C(C=C1)C=O
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| InChi Key |
ZRSNZINYAWTAHE-FIBGUPNXSA-N
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| InChi Code |
InChI=1S/C8H8O2/c1-10-8-4-2-7(6-9)3-5-8/h2-6H,1H3/i1D3
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| Chemical Name |
4-(trideuteriomethoxy)benzaldehyde
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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 |
| 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 | 7.1855 mL | 35.9273 mL | 71.8546 mL | |
| 5 mM | 1.4371 mL | 7.1855 mL | 14.3709 mL | |
| 10 mM | 0.7185 mL | 3.5927 mL | 7.1855 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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