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Description

🧪 Product Profile: Tesamorelin

Product Name: Tesamorelin
CAS Number: 218949-48-5
Molecular Formula: C₂₂₁H₃₆₆N₇₂O₆₇S
Molecular Weight: ~5.1 kDa (44 amino acids)
Amino Acid Sequence: trans-3-hexenoyl-Tyr-Ala-Asp-Ala-Ile-Phe-Thr-Asn-Ser-Tyr-Arg-Lys-Val-Leu-Gly-Gln-Leu-Ser-Ala-Arg-Lys-Leu-Leu-Gln-Asp-Ile-Met-Ser-Arg-Gln-Gln-Gly-Glu-Ser-Asn-Gln-Glu-Arg-Gly-Ala-Arg-Ala-Arg-Leu-NH₂
Purity: ≥98% (HPLC verified)
Formulation: Lyophilized powder (standard vials: 1mg, 5mg, 10mg)

🔬 Key Characteristics

Tesamorelin is a synthetic analog of human growth hormone-releasing hormone (GHRH) featuring an N-terminal trans-3-hexenoyl fatty acid modification. This lipophilic moiety enhances metabolic stability and prolongs half-life (~2 hours) compared to native GHRH, enabling sustained growth hormone (GH) secretion in preclinical models. Originally developed as TH9507, its 44-amino acid sequence retains the full biological activity of endogenous GHRH while resisting enzymatic degradation through structural optimization.

⚙️ Mechanism of Action

• GHRH Receptor Agonism: Binds to pituitary GHRH receptors, activating adenylate cyclase and cAMP signaling to stimulate pulsatile GH release.
• Lipophilic Modification: The trans-3-hexenoyl group increases plasma protein binding, reducing renal clearance and extending systemic exposure.
• IGF-1 Mediation: Induces downstream insulin-like growth factor-1 (IGF-1) production, promoting anabolic effects on muscle, bone, and metabolism.
• Minimal Desensitization: Sustained but physiological GH secretion avoids pituitary receptor downregulation seen with continuous GHRH exposure.

📊 Research Applications

• Endocrinology: Studies on GH deficiency, somatotropic axis regulation, and age-related hormonal decline.
• Metabolic Research: Investigation of visceral fat reduction, insulin sensitivity, and lipid metabolism in obesity models.
• Clinical Translation: Preclinical evaluation for growth disorders, sarcopenia, and HIV-associated lipodystrophy.
• Pharmacokinetic Studies: Analysis of fatty acid-modified peptides for optimized drug delivery and half-life extension.

💡 Product Features

• Stability: Lyophilized form stable for 24 months at 2-8°C; reconstituted solutions (sterile saline) stable for 72 hours under refrigeration.
• Bioactivity: Specific activity ≥5.0×10⁴ IU/mg (rat pituitary cell GH release assay), with ED₅₀ ≤10 nM.
• Selectivity: High affinity for GHRH receptors (Kd ~0.3 nM) with minimal cross-reactivity to other hypothalamic receptors.
• Formulation Flexibility: Available as lyophilized powder or pre-formulated solutions for in vitro and in vivo research applications.

⚠️ Disclaimer

For Research Use Only: Not approved for human or veterinary clinical applications. Handling requires compliance with peptide research protocols, including proper reconstitution, storage, and biosafety measures.

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