Description

Technical Parameters

Introduction

peptides

product-1400-1400

Products Description

#### **1. Overview and Background**

**N-Acetyl Epitalon Amidate** is a chemically modified synthetic tetrapeptide, whose parent molecule is **Epitalon** (also known as **Epithalon** or **Epithalamin**, sequence: **Ala-Glu-Asp-Gly**). Through **N-acetylation** (acetylation of the N-terminal amino group) and **C-amidation** (amidation of the C-terminal carboxylic acid group), the stability, bioavailability and pharmacological activity of the peptide are significantly improved, making it a hot molecule in the field of anti-aging and cell protection research.

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#### **2. Chemical structure and modification category**

##### **1. Basic structure**

- **Original sequence**: Ala-Glu-Asp-Gly (molecular weight: ~390 Da).

- **Modification characteristics**:

- **N-acetylation**: The amino group of the N-terminal alanine (Ala) is replaced by an acetyl group (CH₃CO-), which reduces enzymatic hydrolysis and enhances hydrophobicity.

- **C-amidation**: The carboxylic acid group of C-terminal glycine (Gly) is converted to amide (-CONH₂), which improves the ability to resist degradation by carboxypeptidase.

##### **2. Structural classification**

According to the modification type, Epitalon derivatives can be divided into:

- **Single modification**: Only N-acetylation or C-amidation (such as N-Acetyl Epitalon or Epitalon Amidate).

- **Double modification**: Simultaneous acetylation and amidation (i.e. N-Acetyl Epitalon Amidate), comprehensive optimization of stability and activity.

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#### **3. Physical and chemical properties**

##### **1. Basic physicochemical parameters**

- **Molecular formula**: C₁₈H₂₇N₅O₉ (needs to be calculated according to the specific modification).

- **Molecular weight**: about **490-510 Da** (the exact value needs to be confirmed by mass spectrometry).

- **Solubility**:

- **Water solubility**: Moderate (needs acidic buffer or ultrasound-assisted dissolution).

- **Organic solvents**: Soluble in DMSO and DMF, insoluble in non-polar solvents (such as ether).

- **Stability**:

- **Thermal stability**: Long-term storage at -20°C; easy to degrade at room temperature, need to be dried away from light.

- **pH sensitivity**: Stable in the pH range of 4-7, strong acid/base conditions lead to hydrolysis.

##### **2. Analytical characteristics**

- **HPLC purity**: >95% (C18 reverse phase chromatography, gradient elution).

- **Mass spectrometry characteristics**: ESI-MS shows [M+H]⁺ peak, matching the theoretical molecular weight.

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#### **4. Color and appearance**

- **Solid state**: White to off-white lyophilized powder (when high purity).

- **Solution color**: Colorless and transparent (pH neutral), if yellowing may indicate oxidation or impurities.

- **Influencing factors**:

- **Purity**: Impurities (such as oxidation products) may cause a slightly yellowish color.

- **Storage conditions**: Light or high temperature accelerates degradation and deepens the color.

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#### **5. Biological advantages and functions**

##### **1. Anti-aging and telomere regulation**

- **Telomerase activation**: Delaying telomere shortening by inducing telomerase reverse transcriptase (TERT) expression.

- **Cell life extension**: Prolonging the fibroblast division cycle in an in vitro model.

##### **2. Antioxidant and anti-inflammatory**

- **ROS scavenging**: Inhibits mitochondrial oxidative stress and reduces MDA (malondialdehyde) levels.

- **NF-κB pathway inhibition**: Reduces the release of inflammatory factors (such as IL-6, TNF-α).

##### **3. Immune regulation**

- **Thymus function enhancement**: Promotes T cell differentiation and improves the immune function of elderly animals.

##### **4. Metabolic regulation**

- **SIRT1 activation**: simulates the effect of calorie restriction and improves glucose and lipid metabolism.

##### **5. Neuroprotection**

- **Upregulation of neurotrophic factors**: such as BDNF, may improve cognitive function.

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#### **6. Application areas**

##### **1. Scientific research**

- **Aging mechanism research**: used for telomere dynamics and epigenetic regulation models.

- **Drug development**: used as a lead compound to optimize anti-aging drugs.

##### **2. Preclinical research**

- **Animal model**: prolongs the lifespan of mice and improves age-related diseases (such as osteoporosis).

##### **3. Cosmetics and functional medicine**

- **Anti-aging skin care products**: topical application may reduce skin photoaging.

- **Regenerative medicine**: combined with stem cell therapy to promote tissue repair.

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#### **7. Synthesis and quality control**

##### **1. Synthesis process**

- **Solid phase synthesis (SPPS)**: Fmoc/t-Bu strategy, sequentially connecting amino acids.

- **Purification steps**: HPLC preparation, ion exchange chromatography to remove impurities.

##### **2. Quality control standards**

- **Identification**: Mass spectrometry (MS), nuclear magnetic resonance (NMR).

- **Purity detection**: HPLC ≥ 98%, residual solvents meet ICH standards.

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#### **8. Safety and challenges**

- **Toxicity data**: No significant acute toxicity was observed in animal experiments (LD₅₀>1000 mg/kg).

- **Challenges**:

- **Membrane permeability**: A carrier (such as liposomes) is required to enhance cell permeability.

- **Long-term effects**: More clinical data are needed to verify safety.

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#### **9. Future Outlook**

- **Structural Optimization**: Develop derivatives that penetrate the blood-brain barrier (such as palmitoylation modification).

- **Peptide Combination Therapy**: Combined with NAD+ precursors (such as NMN) for synergistic anti-aging.

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### **Conclusion**

N-Acetyl Epitalon Amidate has become an important tool for biomedical research due to its unique chemical modification and multi-target anti-aging mechanism. With the advancement of synthetic technology and the deepening of clinical transformation, its potential in the field of extending healthy life span is worth looking forward to.