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| Targets |
Telomerase; anti-aging
The primary target of Epitalon is telomerase, the ribonucleoprotein complex that adds telomeric repeats to chromosome ends. Epitalon activates telomerase expression, leading to telomere elongation and increased cellular lifespan. It also targets genes involved in cell cycle regulation, apoptosis, and antioxidant defense, though the precise molecular receptor for the tetrapeptide has not been definitively identified. |
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| ln Vitro |
The enzymatic activity of telomerase, telomere elongation, and catalytical subunit expression were all induced by the addition of Epithalon peptide in telomerase-negative human fetal fibroblast culture. This phenomenon may be the result of somatic cell reactivation of the telomerase gene, and it suggests that extending the lifespan of individual cells and the organism as a whole is possible[1].
In vitro, Epitalon induces telomerase activity in telomerase-negative human fetal fibroblast cultures, leading to telomere elongation and expression of the catalytic subunit (hTERT). This phenomenon suggests reactivation of the telomerase gene in somatic cells, potentially extending the lifespan of individual cells and entire organisms. Epitalon also enhances the proliferative capacity of various cell types and reduces markers of cellular senescence. |
| ln Vivo |
In addition to extending the lives of fruit flies and mice, epitalon TFA also helps aged rhesus monkeys regain their circadian rhythms of cortisol and melatonin production. In addition, Epitalon enhances visual functions in patients suffering from pigmental retinal degeneration and prolongs the functional integrity of the eye retina in Campbell rats with hereditary Retinitis Pigmentosa[1]. The subcutaneous injection of epitalon TFA (1.0 µg/mouse (30–40 µg/kg); administered five days a month for three to twelve months) has no effect on the average lifespan, body weight, or food intake of mice. On the other hand, Epitalon reduces the incidence of chromosome abnormalities in bone marrow cells by 17.1% and slows down the age-related switching off of estrous activity. In Swiss-derived SHR mice, epitalon extended the life span of the final 10% of survivors by 13.3% when compared to the control group[4].
In vivo, Epitalon inhibits the development of spontaneous tumors in mice and exhibits geroprotective effects. It increases neuronal activity when administered intranasally and is indicated for cancer, aging, and retinitis pigmentosa research. Subcutaneous injection of Epitalon (1.0 ug/mouse, approximately 30-40 ug/kg, monthly for 3-12 months) reduces the incidence of chromosomal aberrations in bone marrow cells by 17.1% and slows age-related cessation of estrous activity. In Swiss-derived SHR mice, Epitalon extends the lifespan of the last 10% of survivors by 13.3% compared to controls. Epitalon restores circadian rhythms of melatonin and cortisol production in aged rhesus monkeys and enhances visual function in patients with retinitis pigmentosa. It extends the lifespan of mice and fruit flies. |
| Enzyme Assay |
For cell-free binding studies, as a tetrapeptide, Epitalon does not have a classical receptor in cell-free systems. For telomerase activity assays, prepare cell lysates from treated cells. Assay telomerase activity using TRAP (Telomeric Repeat Amplification Protocol): extract protein lysates from control or Epitalon-treated cells, amplify using the TRAP assay kit, resolve PCR products on a polyacrylamide gel, and visualize by silver staining or SYBR Green. A characteristic 6-bp ladder indicates telomerase activity. For quantitative analysis, use real-time TRAP (qTRAP).
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| Cell Assay |
Culture human fetal fibroblasts or telomerase-negative cell lines in DMEM with 10% FBS and 1% penicillin/streptomycin at 37degC with 5% CO2. Add Epitalon TFA to culture medium at concentrations of 0.1-100 uM for 7-28 days. For telomerase activity measurement, harvest cells, lyse, and perform TRAP assay as described. For telomere length measurement, extract DNA and perform Southern blot or quantitative PCR (qPCR) for telomere repeat copy number relative to a single-copy gene (T/S ratio). Assess cell proliferation by CCK-8 or cell counting. Measure cellular senescence by senescence-associated beta-galactosidase (SA-beta-Gal) staining at pH 6.0. Assess apoptosis by flow cytometry using Annexin V/PI staining.
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| Animal Protocol |
Animal/Disease Models: Swiss-derived SHR mice[4]
Doses: 1.0 µg/mouse (∼30-40 µg/kg) Route of Administration: subcutaneous (sc) injection ; 1.0 µg/mouse (∼30-40 µg/kg) ; 5 days every month; 3-12 months Experimental Results: Dramatically diminished the age-associated increase in chromosome aberrations after long-term treatment. For geroprotection studies, use Swiss-derived SHR mice or C57BL/6 mice. Administer Epitalon TFA via subcutaneous (SC) injection at 1.0 ug/mouse (approximately 30-40 ug/kg) or intranasal (IN) administration (5-10 ug/mouse). Dosing schedule: 5 consecutive days each month, for 3-12 months. For lifespan studies, monitor mice daily for mortality and calculate median and maximum lifespan (last 10% survivors). For tumor studies, assess spontaneous tumor development by necropsy at end of study. For neuroactivity studies, administer intranasally (10-50 ug/kg) and assess behavior in open field or elevated plus maze. For retinitis pigmentosa models, use Campbell rats with hereditary retinitis pigmentosa, treat with Epitalon, and assess retinal function by electroretinography (ERG). Collect blood and tissues for histology, biochemistry, and molecular analyses. |
| ADME/Pharmacokinetics |
Epitalon is a tetrapeptide that is likely subject to rapid proteolytic degradation in the gastrointestinal tract and circulation, making oral bioavailability low. Intranasal administration provides direct delivery to the central nervous system and bypasses first-pass metabolism. Subcutaneous injection results in systemic distribution. Plasma half-life in rodents is expected to be short (minutes to a few hours) for the free peptide. TFA salt form enhances water solubility and formulation stability.
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| Toxicity/Toxicokinetics |
Epitalon has a favorable safety profile with minimal toxicity reported in preclinical studies. Subcutaneous administration of Epitalon at 1.0 ug/mouse had no effect on average lifespan, body weight, or food intake of mice. Long-term treatment dramatically diminished the age-associated increase in chromosome aberrations. The compound is not associated with genotoxicity or carcinogenicity in animal models. Material safety data sheets indicate that TFA salts may cause irritation; standard laboratory precautions (gloves, lab coat, safety glasses) should be used.
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| References | |
| Additional Infomation |
The addition of Epithalon peptide to telomerase-negative human fetal fibroblast cultures induced expression of telomerase catalytic subunits, enzyme activity, and telomere elongation, which may be due to the reactivation of telomerase genes in somatic cells and suggests the potential to extend the lifespan of cell populations and the entire organism. [3]
Epitalon is also known as Epithalon, Epithalamin, or Epithalone. The tetrapeptide sequence is H-Ala-Glu-Asp-Gly-OH (AEDG). The TFA salt form has molecular weight 504.37 and formula C16H23F3N4O11. Epitalon is included in some anti-aging supplements, though its clinical use remains investigational. It has been studied in clinical trials for retinitis pigmentosa, cancer, and aging-related conditions. The compound is exclusively for research use. |
| Molecular Formula |
C16H23F3N4O11
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|---|---|
| Molecular Weight |
504.37
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| Exact Mass |
504.1315420
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| Related CAS # |
Epitalon;307297-39-8
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| PubChem CID |
145712429
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| Sequence |
L-alanyl-L-alpha-glutamyl-L-alpha-aspartyl-glycine trifluoroacetic acid; H-Ala-Glu-Asp-Gly-OH.TFA
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| SequenceShortening |
AEDG
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| Appearance |
Typically exists as solid at room temperature
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| Hydrogen Bond Donor Count |
8
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| Hydrogen Bond Acceptor Count |
15
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| Rotatable Bond Count |
12
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| Heavy Atom Count |
34
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| Complexity |
691
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| Defined Atom Stereocenter Count |
3
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| SMILES |
C[C@@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)O)N.C(=O)(C(F)(F)F)O
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| InChi Key |
RJCJYCJZMHAFCM-WQYNNSOESA-N
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| InChi Code |
InChI=1S/C14H22N4O9.C2HF3O2/c1-6(15)12(25)17-7(2-3-9(19)20)14(27)18-8(4-10(21)22)13(26)16-5-11(23)24;3-2(4,5)1(6)7/h6-8H,2-5,15H2,1H3,(H,16,26)(H,17,25)(H,18,27)(H,19,20)(H,21,22)(H,23,24);(H,6,7)/t6-,7-,8-;/m0./s1
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| Chemical Name |
(4S)-4-[[(2S)-2-aminopropanoyl]amino]-5-[[(2S)-3-carboxy-1-(carboxymethylamino)-1-oxopropan-2-yl]amino]-5-oxopentanoic acid;2,2,2-trifluoroacetic acid
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| Synonyms |
Epitalon (TFA); Epithalon TFA;
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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. |
| 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 :~250 mg/mL (~495.67 mM)
H2O :~100 mg/mL (~198.27 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.12 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 20.8 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: ≥ 2.08 mg/mL (4.12 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 20.8 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: ≥ 2.08 mg/mL (4.12 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 50 mg/mL (99.13 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9827 mL | 9.9134 mL | 19.8267 mL | |
| 5 mM | 0.3965 mL | 1.9827 mL | 3.9653 mL | |
| 10 mM | 0.1983 mL | 0.9913 mL | 1.9827 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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