| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg | |||
| 50mg | |||
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| Other Sizes |
Purity: =98.86%
| Targets |
Telomerase
Epithalon's primary mechanism of action is the induction of telomerase activity and telomere elongation in human somatic cells. By up-regulating telomerase, the enzyme responsible for maintaining telomere length, Epithalon helps preserve genomic stability and cellular replicative capacity. It can penetrate the cell membrane and enter the nucleus, where it increases the transcriptional levels of neurogenesis-related genes such as Nestin and GAP43. Epithalon also modulates melatonin and cortisol production, influencing circadian rhythms. |
|---|---|
| ln Vitro |
The addition of Epithalon peptide to telomerase-negative human fetal fibroblast culture resulted in the expression of the catalytical subunit, enzymatic activity of telomerase, and telomere elongation. This suggests that the telomerase gene may have been reactivated in somatic cells and may lead to an extension of the life span of both cell populations and the entire organism[1].
In vitro, Epithalon treatment at 0.01 µg/ml for 7 days significantly upregulates the expression of neurogenesis-related genes and the synthesis of β-tubulin III and Doublecortin in human gingival mesenchymal stem cells (hGMSCs). Treatment with 50 nM Epithalon for 24 hours prevents the decrease in neprilysin and insulin-degrading enzyme expression induced by hypoxia in NB7 neuroblastoma cells. At 400 ng/ml for 24 hours, it alleviates UV-induced oxidative stress and increases the expression of SOD-1, NQO1, and CATALASE genes in dermal fibroblasts. |
| ln Vivo |
Epitalon prolongs the life of fruit flies and mice, and it helps elderly rhesus monkeys' circadian rhythms of cortisol and melatonin production to return. 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].
In vivo, Epithalon treatment via oral administration at a dose of 100 µg/day for one month significantly improves the transport properties of the small intestine in aged rats and promotes active glucose accumulation in the proximal and distal segments of the small intestine. Epithalon (1 µg) administered subcutaneously five times a week for six months significantly suppresses tumor growth in female transgenic FVB/N mice carrying the breast cancer gene HER-2/neu. It also extends replicative lifespan by approximately 10 population doublings in human fibroblasts. |
| Enzyme Assay |
Non-cellular assays for Epithalon are limited, as it is a peptide that acts through intracellular signaling pathways. Its ability to induce telomerase activity can be assessed in cell-free systems using telomerase repeat amplification protocol (TRAP) assays with cellular extracts treated with the peptide. The binding of Epithalon to potential targets can be studied using surface plasmon resonance (SPR) or isothermal titration calorimetry (ITC) to characterize its interactions with specific proteins or DNA sequences.
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| Cell Assay |
In vitro cellular assays for Epithalon involve treating human somatic cells (e.g., fibroblasts, gingival mesenchymal stem cells) with the compound and measuring telomerase activity, telomere length, and gene expression. Telomerase activity is measured using the TRAP assay, while telomere length is assessed by quantitative PCR or Southern blot analysis. The expression of neurogenesis-related and antioxidant genes is quantified by qPCR or Western blotting. Cell proliferation and senescence are evaluated using population doubling assays and β-galactosidase staining.
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| Animal Protocol |
In vivo animal experiments with Epithalon are conducted in aged rodent models and transgenic cancer models. Aged rats are treated with Epithalon via oral administration at doses of 100 µg/day for one month, and the transport properties of the small intestine and glucose accumulation are assessed. In tumor models, female transgenic FVB/N mice carrying the HER-2/neu breast cancer gene are treated subcutaneously with 1 µg Epithalon five times a week for six months, and tumor growth is monitored. Life extension studies are conducted to assess the compound's effects on maximum lifespan.
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| ADME/Pharmacokinetics |
Epithalon has a molecular weight of 390.35 and a molecular formula of C₁₄H₂₂N₄O₉. It is a solid powder with a purity of ≥98%. The compound is soluble in DMSO and is typically stored at -20°C. It is stable under recommended storage conditions. The tetrapeptide sequence is Ala-Glu-Asp-Gly (AEDG).
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| Toxicity/Toxicokinetics |
Epithalon is a research compound for laboratory use only and is not approved for human therapeutic or diagnostic use. In preclinical studies, it has been generally well-tolerated at the doses used for efficacy studies. As a peptide, it may have low immunogenicity potential. Standard laboratory safety precautions should be followed when handling the compound. It may cause skin, eye, and respiratory irritation.
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| References | |
| Additional Infomation |
Epitalon is an organic molecular entity.
The addition of Epitalon peptide to telomerase-negative human fetal fibroblast cultures induces expression of catalytic subunits, telomerase 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] Epithalon (CAS 307297-39-8) is a synthetic tetrapeptide (Ala-Glu-Asp-Gly) that induces telomerase activity and telomere elongation. It is based on the amino acid composition of the pineal polypeptide Epithalamin. Epithalon has anti-aging, geroprotective, and potential anticancer properties. It modulates melatonin and cortisol production and regulates the cell cycle. The compound is primarily used in gerontology and regenerative medicine research. |
| Molecular Formula |
C14H22N4O9
|
|---|---|
| Molecular Weight |
390.35
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| Exact Mass |
390.138
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| Elemental Analysis |
C, 43.08; H, 5.68; N, 14.35; O, 36.89
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| CAS # |
307297-39-8
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| Related CAS # |
Epitalon TFA; 307297-40-1 (acetate)
|
| PubChem CID |
219042
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| Sequence |
H-Ala-Glu-Asp-Gly-OH; L-alanyl-L-alpha-glutamyl-L-alpha-aspartyl-glycine
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| SequenceShortening |
AEDG
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
959.8±65.0 °C at 760 mmHg
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| Flash Point |
534.3±34.3 °C
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| Vapour Pressure |
0.0±0.6 mmHg at 25°C
|
| Index of Refraction |
1.559
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| LogP |
-2.02
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| Hydrogen Bond Donor Count |
7
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
12
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| Heavy Atom Count |
27
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| Complexity |
607
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| Defined Atom Stereocenter Count |
3
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| SMILES |
OC(CNC([C@@H](NC([C@@H](NC([C@@H](N)C)=O)CCC(=O)O)=O)CC(=O)O)=O)=O
|
| InChi Key |
HGHOBRRUMWJWCU-FXQIFTODSA-N
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| InChi Code |
InChI=1S/C14H22N4O9/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/h6-8H,2-5,15H2,1H3,(H,16,26)(H,17,25)(H,18,27)(H,19,20)(H,21,22)(H,23,24)/t6-,7-,8-/m0/s1
|
| Chemical Name |
(4S)-4-[[(2S)-2-aminopropanoyl]amino]-5-[[(2S)-3-carboxy-1-(carboxymethylamino)-1-oxopropan-2-yl]amino]-5-oxopentanoic acid
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| Synonyms |
AlaGluAspGly;
Epitalon; 307297-39-8; Epithalon; Epithalone; Ala-Glu-Asp-Gly; Epithalon
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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: ≥ 50 mg/mL (~128.1 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 | 2.5618 mL | 12.8090 mL | 25.6180 mL | |
| 5 mM | 0.5124 mL | 2.5618 mL | 5.1236 mL | |
| 10 mM | 0.2562 mL | 1.2809 mL | 2.5618 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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