Testagen 20mg

Compound Name: Testagen

Synonyms: KEDG

CAS Number: N/A; Not registered

Molecular Formula: C₁₇H₂₉N₅O₉

Molecular Weight: ~ 447.44 g/mol

Structure: Synthetic tetrapeptide

Peptide Sequence: H-Lys-Glu-Asp-Gly-OH

Chemical Structure:

Source: PubChem

Mechanism of Action: Testagen exerts its regulatory effects by penetrating cells and binding directly to DNA promoter regions, particularly CAG- or CG-rich sequences. This site-specific interaction prevents DNA methyltransferase activity, ensuring continued expression of genes critical for protein and hormone synthesis in the testes. At the cellular level, Testagen stimulates biosynthesis of cytoskeletal (actin, vimentin) and nuclear (lamin A/C) proteins that support Leydig cell structure and function, maintains chromatin in a transcriptionally active state, and suppresses apoptosis in steroidogenic cell populations^1-4.

Biological Activity: In preclinical models, Testagen promotes proliferation and function of testicular cells, supports differentiation of stem/progenitor cells into reproductive and endocrine tissue phenotypes, and enhances protein synthesis in organs undergoing age-related regression, including the testes^1,2,4. It has been shown to improve the morphofunctional state of endocrine tissues, potentially contributing to sustained hormone output. While not a direct testosterone analog, its epigenetic and cellular effects may, in research contexts, help maintain favorable conditions for endogenous testosterone synthesis³.

Storage: Store lyophilized at −20 °C; reconstituted solutions at 2–8 °C, use within 4 weeks. Avoid repeated freeze-thaw.

Drug Categories: Peptide bioregulator; experimental geroprotector; endocrine regulator

Additional Notes: N/A

Summary Table:

Disclaimer: For Research Use Only. Not intended for human or veterinary use. This compound is supplied solely for laboratory and R&D purposes.

Detailed Product Description

Testagen is a tetrapeptide engineered to modulate the functional activity of the testes and associated endocrine glands. Through epigenetic modulation, it maintains transcriptional activity in key hormone synthesis pathways and enhances the cellular architecture required for effective steroidogenesis. In aging models, Testagen restores structural integrity, protein synthesis, and metabolic activity in endocrine tissues that support testosterone production. In vitro, it has been shown to upregulate the structural proteins that maintain Leydig cell viabilty and increase the accessibility of genome regions controlling steroidogenic enzymes^1,3. These research findings indicate that Testagen may be a valuable model compound for studying physiological testosterone regulation, particularly in the context of aging or functional decline^2,4.

Research Highlights

• Endocrine and Testosterone Support: Regulates testicular function by maintaining chromatin in a transcriptionally active state, preventing promoter methylation of steroidogenesis-related genes, stimulating protein synthesis in Leydig cells, supporting cholesterol transport mechanisms, and reducing apoptosis in hormone-producing cells, thereby sustaining endogenous testosterone biosynthetic capacity in experimental models^1,3,4.

• Stem Cell Differentiation and Immune Enhancement: Promotes the differentiation of CD34⁺ stem/progenitor cells into T lymphocytes and other immune-active phenotypes, increases proliferation of mature T-cells, and modifies cell receptor expression patterns to enhance immune adaptability; these effects may indirectly support endocrine–immune cross-talk and hormone homeostasis¹.

• Epigenetic Gene Regulation: Demonstrated to bind selectively to CAG- and CG-rich promoter sites, shielding them from DNA methyltransferase activity, maintaining unmethylated status, upregulating “silent” genes, and enabling sustained transcription of proteins and enzymes critical for reproductive function and cell longevity^1,2.

• Cellular Structure and Function Preservation: Increases cytoskeletal (actin, vimentin) and nuclear (lamin A/C) protein synthesis to reinforce cellular architecture in endocrine tissues, maintains optimal microenvironment for steroid production, and counteracts age-related involution of reproductive organs^1,2,4.

• Anti-Apoptotic and Cytoprotective Action: Suppresses mitochondrial-dependent apoptosis in hormone-producing and progenitor cell populations, promoting long-term viability of functional endocrine cells and supporting sustained anabolic and androgenic activity².

Mechanism of Action

Epigenetic Activation of Steroidogenesis Genes

• Selectively binds to promoter regions of genes coding for key steroidogenic enzymes (e.g., StAR, CYP11A1)^1,3.
• Prevents methylation-induced silencing, enabling persistent transcription and hormone synthesis^2,4.
• May indirectly enhance testosterone output under research conditions by sustaining enzyme expression^1,2.

Cytoskeletal and Nuclear Support of Leydig Cells

• Increases actin, vimentin, and lamin A/C synthesis, maintaining Leydig cell structure and optimal hormone production environment^1,3.
• Supports transport and processing of cholesterol substrates in steroidogenic cells².

Anti-Apoptotic Protection of Endocrine Tissue

• Inhibits mitochondrial apoptosis pathways in hormone-producing cells¹.
• Preserves functional cell populations conducive to testosterone synthesis³.

Pharmacokinetic Profile

• Route of Administration: Intravenous injection (IV), transdermal patch
• Dosing Frequency: Once daily
• Half-Life: ~5-20 hours (route dependent, shorter for intravenous)

Formulation & Handling

• Store in tightly sealed containers, protected from light
• Use only for authorized research or laboratory applications

Selected Clinical Trial Activity

References

¹Khavinson, V.K. et al. Morphofunctional fundamentals for peptide regulation of aging. Biol. Bull. Rev. 1, 3–15 (2011).

²Khavinson, V.K. et al. Mechanism of biological activity of short peptides: cell penetration and epigenetic regulation of gene expression. Biol. Bull. Rev. 3, 450–467 (2013).

³Khavinson, V.K. et al. Epigenetic aspects of peptide-mediated regulation of aging. Adv. Gerontol. 25, 11–26 (2012).

⁴Kuznik, B.I., Pateiuk, A.V., Rusaeva, N.S., Baranchugova, L.M. & Obydenko, V.I. Effects of Lys–Glu–Asp–Gly and Ala–Glu–Asp–Gly peptides on hormonal activity and thyroid morphology in hypophysectomized mature and old birds. Adv. Gerontol. 24, 93–98 (2011).