Epitalon TFA is an anti-aging agent and telomerase activator. Epitalon TFA inhibits the development of spontaneous tumors in mice, has geroprotective effects, and increases neuronal activity through intranasal administration. Epitalon TFA is indicated for cancer, aging and retinitis pigmentosa.

Physicochemical Properties

Molecular Formula	C16H23F3N4O11
Molecular Weight	504.37
Related CAS #	Epitalon;307297-39-8
Appearance	Typically exists as solid at room temperature
HS Tariff Code	2934.99.9001
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)

Biological Activity

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].
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].
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.
References	[1]. Peptides and Ageing. Neuro Endocrinol Lett. 2002;23 Suppl 3:11-144. [2]. Identification of the small research tetra peptide Epitalon, assumed to be a potential treatment for cancer, old age and Retinitis Pigmentosa in two illegal pharmaceutical preparations. Drug Test Anal. 2015 Mar;7(3):259-64. [3]. Epithalon peptide induces telomerase activity and telomere elongation in human somatic cells. Bull Exp Biol Med. 2003 Jun;135(6):590-2. [4]. Effect of Epitalon on biomarkers of aging, life span and spontaneous tumor incidence in female Swiss-derived SHR mice. Biogerontology. 2003;4(4):193-202.

Solubility Data

Solubility (In Vitro)

DMSO :~250 mg/mL (~495.67 mM) H2O :~100 mg/mL (~198.27 mM)

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. 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. 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 corn oil and mix evenly. 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.  (Please use freshly prepared in vivo formulations for optimal results.)

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.