Epitalon

Research Overview

Epitalon serves as a valuable research tool for investigating cellular aging mechanisms and circadian rhythm regulation in laboratory settings. This synthetic tetrapeptide was developed by Russian scientist Professor Vladimir Khavinson based on epithalamin, a natural pineal gland extract containing multiple peptides. Epitalon represents the active tetrapeptide component identified through isolation and characterization studies of epithalamin’s biological activities.

The peptide’s designation stems from epithalamin-like properties, reflecting its origin as a synthetic version of the naturally occurring pineal peptide. Research applications have expanded to encompass telomere biology, cellular senescence mechanisms, and neuroendocrine regulation investigations. Laboratory studies examine Epitalon’s effects on telomerase enzyme activity, telomere length maintenance, pineal gland hormone secretion, and age-related cellular changes.

Epitalon research demonstrates the peptide’s potential to influence fundamental aging mechanisms at the cellular level. Studies have documented effects on telomerase reverse transcriptase (TERT) expression, telomere elongation processes, and pineal melatonin production patterns. Research protocols examine these effects in cell culture systems, tissue preparations, and preclinical animal models across multiple species.

Molecular Characteristics

Complete Specifications:

• CAS Registry Number: NOT ASSIGNED (synthetic peptide)
• Molecular Weight: 307.3 Da
• Molecular Formula: C₁₄H₂₂N₄O₉
• Amino Acid Sequence: Ala-Glu-Asp-Gly (AEDG)
• Peptide Classification: Synthetic tetrapeptide
• Appearance: White to off-white lyophilized powder
• Solubility: Water, bacteriostatic water, phosphate buffered saline

The peptide’s four-amino acid structure provides a compact, easily synthesized research tool. The sequence includes two acidic residues (glutamic acid, aspartic acid) contributing to negative charge at physiological pH, along with neutral alanine and glycine residues. This composition influences solubility characteristics and potential interactions with cellular targets. The relatively small molecular weight facilitates membrane permeability studies and cellular uptake investigations.

Pharmacokinetic Profile in Research Models

Epitalon pharmacokinetic characterization in preclinical research reveals important properties for experimental design:

Absorption and Bioavailability:

• Multiple administration routes investigated: subcutaneous, intraperitoneal, intravenous
• Peptide shows systemic bioavailability following parenteral administration
• Small molecular size may facilitate cellular membrane crossing
• Oral bioavailability limited by peptidase degradation (typical for short peptides)

Distribution and Elimination:

• Rapid distribution following systemic administration
• Plasma half-life estimated at 30-90 minutes (varies by species and route)
• Tissue distribution patterns under investigation in research models
• Renal clearance pathway predominant for small peptides

Biological Activity Timeline:

• Acute effects observed within hours of administration in some models
• Chronic effects on telomere length require extended study periods (weeks to months)
• Telomerase activation detected 24-72 hours post-administration in cell studies
• Melatonin modulation effects observed with repeated administration protocols

These pharmacokinetic characteristics inform research protocol design, particularly regarding dosing frequency, study duration, and sample collection timing in experimental models.

Research Applications

Telomere Biology and Telomerase Research

Epitalon serves as a research tool for investigating telomere dynamics and telomerase regulation:

• Telomerase Activity Studies: Investigation of telomerase reverse transcriptase (TERT) gene expression and enzyme activity modulation
• Telomere Length Analysis: Research on telomere elongation mechanisms and maintenance processes
• Cellular Senescence Research: Examination of replicative senescence pathways and senescence-associated markers
• Cell Cycle Regulation: Studies on proliferative capacity and cell division potential in various cell types
• Chromosome Stability Research: Investigation of telomere-mediated chromosome protection mechanisms

Research protocols employ telomere restriction fragment (TRF) analysis, telomerase repeat amplification protocol (TRAP) assays, quantitative PCR for telomere length assessment, and fluorescence in situ hybridization (FISH) techniques. Studies examine effects in primary cell cultures, immortalized cell lines, and tissue samples from animal models.

Pineal Gland and Circadian Rhythm Research

Given Epitalon’s origin from pineal gland extracts, substantial research focuses on neuroendocrine applications:

• Melatonin Production Studies: Investigation of pineal gland melatonin synthesis and secretion patterns
• Circadian Rhythm Research: Analysis of circadian clock gene expression and rhythm regulation
• Photoperiod Response Studies: Examination of seasonal adaptation mechanisms and photoperiod-responsive pathways
• Pinealocyte Function Research: Studies on pineal cell activity, hormone production, and regulatory mechanisms
• Neuroendocrine Axis Investigation: Research on hypothalamic-pituitary-pineal interactions

Laboratory studies utilize pineal gland explants, pinealocyte cultures, melatonin measurement assays (ELISA, HPLC), and circadian behavior monitoring in animal models. Research examines both acute and chronic effects on pineal function parameters.

Cellular Aging and Longevity Research

Epitalon investigations extend to fundamental aging mechanism studies:

• Age-Related Gene Expression: Research on genes associated with aging processes and longevity pathways
• Oxidative Stress Research: Studies examining antioxidant enzyme expression and oxidative damage markers
• Mitochondrial Function Studies: Investigation of mitochondrial biogenesis, respiration, and age-related changes
• Protein Synthesis Research: Analysis of protein production capacity and age-related protein modifications
• Cellular Repair Mechanisms: Examination of DNA repair pathways and cellular maintenance processes

Experimental models include young vs. aged animal comparisons, accelerated aging models, and longitudinal studies examining age-related biomarkers over time.

Neuroendocrine System Research

Research applications encompass broader neuroendocrine regulation studies:

• Hormone Regulation Research: Investigation of various endocrine axes and hormone production patterns
• Hypothalamic Function Studies: Examination of hypothalamic peptide production and regulatory mechanisms
• Pituitary Axis Research: Studies on pituitary hormone secretion and feedback regulation
• Gonadal Function Research: Investigation of reproductive hormone pathways and age-related changes
• Thyroid Function Studies: Research on thyroid hormone production and metabolic regulation

Laboratory protocols investigate hormone levels through immunoassays, gene expression analysis of hormone-producing tissues, and functional assessments in endocrine research models.

Immune System and Stress Response Research

Emerging research areas include immunological and stress response applications:

• Immune Function Studies: Investigation of immune cell populations, activity, and age-related immunosenescence
• Thymic Function Research: Examination of thymus gland involution and T-cell production
• Stress Adaptation Studies: Research on cortisol regulation, stress response pathways, and resilience mechanisms
• Inflammatory Marker Research: Analysis of cytokine profiles and inflammatory pathway modulation
• Adaptive Response Studies: Investigation of cellular stress resistance and adaptive capacity

Research employs flow cytometry for immune cell analysis, cytokine multiplex assays, stress hormone measurements, and behavioral stress models.

Cardiovascular and Metabolic Research

Laboratory studies investigate cardiovascular system applications:

• Vascular Function Studies: Examination of endothelial function, blood pressure regulation, and vascular health markers
• Cardiac Aging Research: Investigation of age-related cardiac changes and cardioprotective mechanisms
• Lipid Metabolism Studies: Research on cholesterol metabolism, lipid profiles, and metabolic regulation
• Glucose Homeostasis Research: Analysis of insulin sensitivity, glucose metabolism, and age-related metabolic changes
• Energy Metabolism Studies: Examination of metabolic rate, energy expenditure, and mitochondrial metabolism

Laboratory Handling and Storage Protocols

Lyophilized Powder Storage:

• Store at -20°C to -80°C in original sealed vial
• Protect from light exposure and moisture
• Desiccated storage environment essential
• Stability data available for 12+ months at -20°C
• Record storage conditions and lot number for research documentation

Reconstitution Guidelines:

• Reconstitute with sterile water, bacteriostatic water (0.9% benzyl alcohol), or appropriate buffer
• Add solvent slowly down vial side to minimize foaming
• Gentle swirling motion recommended (avoid vigorous shaking or vortexing)
• Allow complete dissolution before use (typically 1-3 minutes)
• Final pH should be 6.5-7.5 for optimal stability
• Calculate final concentration based on peptide content (typically 80-85% by weight)

Reconstituted Solution Storage:

• Short-term storage: 4°C for up to 7 days (with bacteriostatic water)
• Long-term storage: -20°C to -80°C in single-use aliquots
• Single-use aliquots strongly recommended to avoid freeze-thaw degradation
• Avoid repeated freeze-thaw cycles (maximum 2 cycles recommended)
• Store in protein low-binding tubes to minimize adsorption losses
• Label aliquots with concentration, date, and lot number

Quality Assurance and Analytical Testing

Each Epitalon batch undergoes comprehensive analytical characterization:

Purity Analysis:

• High-Performance Liquid Chromatography (HPLC): ≥98% purity
• Analytical method: Reversed-phase HPLC with UV detection at 214-220nm
• Multiple peak integration ensures accurate purity determination
• Gradient elution method optimized for tetrapeptide separation

Structural Verification:

• Electrospray Ionization Mass Spectrometry (ESI-MS): Confirms molecular weight 307.3 Da
• Amino acid analysis: Verifies sequence composition (Ala-Glu-Asp-Gly)
• Peptide content determination: Quantifies actual peptide content by weight (typically 80-85%)
• Nuclear Magnetic Resonance (NMR) available for structural confirmation

Contaminant Testing:

• Bacterial endotoxin: <5 EU/mg (LAL method, USP )
• Heavy metals: Below detection limits per USP standards
• Residual solvents: TFA, acetonitrile within ICH Q3C acceptable limits
• Water content: Karl Fischer titration (<8%)
• Bioburden testing for microbial contamination

Documentation:

• Certificate of Analysis (COA) provided with each batch
• Third-party analytical verification available upon request
• Stability data documented for recommended storage conditions
• Batch-specific QC results traceable by unique lot number
• Full analytical raw data available for research documentation

Research Considerations

Experimental Design Factors:

Researchers should consider several factors when designing Epitalon experiments:

1. Concentration Selection: Published research reports concentration ranges from nanomolar to micromolar in cell studies, with dosing in animal models varying by species, route, and research objectives. Dose-response studies recommended for new experimental systems.

2. Temporal Considerations: Telomere effects require extended study periods (weeks to months) while some enzymatic effects may occur more rapidly (hours to days). Study duration should match research question and expected biological timeline.

3. Route Considerations: Subcutaneous and intraperitoneal routes commonly used in animal research. Intravenous administration for pharmacokinetic studies. Route selection should consider research questions and experimental feasibility.

4. Model Selection: Choose appropriate cell culture systems (fibroblasts, immune cells, pinealocytes), tissue explants (pineal gland), or animal models based on specific research questions.

5. Control Groups: Include appropriate vehicle controls, age-matched controls, and positive controls where applicable. Consider time-of-day effects for circadian research.

6. Sample Collection Timing: Plan sample collection based on pharmacokinetics and expected biological effects timeline. Consider circadian variations for neuroendocrine measurements.

Mechanism Investigation:

Epitalon’s mechanisms of action involve multiple potential pathways under active research investigation:

• Telomerase Activation: Proposed mechanisms include TERT gene expression upregulation, telomerase enzyme stabilization, or regulatory factor modulation
• Epigenetic Effects: Potential influence on histone modifications, DNA methylation patterns, or chromatin structure affecting gene expression
• Neuroendocrine Signaling: Possible effects on pineal gland signaling cascades, melatonin synthesis enzymes, or circadian clock proteins
• Gene Expression Modulation: Reported effects on multiple genes associated with aging, stress response, and cellular maintenance
• Antioxidant Pathways: Potential modulation of antioxidant enzyme expression or oxidative stress response mechanisms

The peptide’s multiple potential mechanisms require careful experimental design with appropriate molecular, biochemical, and functional outcome measures to isolate specific effects.

Compliance and Safety Information

Regulatory Status:
Epitalon is provided as a research chemical for in-vitro laboratory studies and preclinical research only. This product has not been approved by the FDA for human therapeutic use, dietary supplementation, or medical applications.

Intended Use:

• In-vitro cell culture studies and biochemical assays
• In-vivo preclinical research in approved animal models
• Laboratory investigation of biological mechanisms
• Academic and institutional research applications
• Mechanism of action studies

NOT Intended For:

• Human consumption or administration
• Therapeutic treatment or diagnosis
• Dietary supplementation or anti-aging products
• Veterinary therapeutic applications without appropriate oversight
• Any medical or clinical applications

Safety Protocols:
Researchers should follow standard laboratory safety practices when handling Epitalon:

• Use appropriate personal protective equipment (lab coat, gloves, safety glasses)
• Handle in well-ventilated areas or biological safety cabinet
• Follow institutional biosafety guidelines and approved protocols
• Dispose of waste according to local regulations for biological/chemical waste
• Consult material safety data sheet (MSDS) for additional safety information
• Follow institutional IACUC protocols for animal research

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