Tesamorelin
Growth Hormone- Molecular Formula
- C221H366N72O67S
- Molar Mass
- 5,135.9 g/mol
- CAS Number
- 218949-48-5
- Purity Standard
- 99%+ (HPLC Verified)
- Amino Acid Sequence
- Trans-3-hexenoic acid-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-Leu-Ser-Arg-Gln-Gln-Gly-Glu-Ser-Asn-Gln-Glu-Arg-Gly-Ala-Arg-Ala-Arg-Leu-NH2
Overview
Tesamorelin is a synthetic analog of human growth hormone-releasing hormone (GHRH) modified with a trans-3-hexenoic acid group at the N-terminus. This modification protects against enzymatic degradation while maintaining full biological activity at the GHRH receptor, resulting in enhanced pharmacokinetic properties compared to native GHRH.
The compound stimulates GH secretion through binding and activation of pituitary GHRH receptors, producing physiological pulsatile GH release. Unlike exogenous GH administration, tesamorelin preserves the negative feedback mechanisms that regulate endogenous GH secretion.
Clinical research has focused particularly on HIV-associated lipodystrophy, where tesamorelin has demonstrated significant reductions in visceral adipose tissue. Studies show approximately 15-18% reduction in trunk fat while preserving subcutaneous fat depots, along with improvements in lipid profiles and patient-reported body image outcomes.
Ongoing research explores tesamorelin's potential in non-alcoholic fatty liver disease (NAFLD), where GH's lipolytic and hepatoprotective effects may provide therapeutic benefit. Studies have shown reductions in liver fat content and improvements in hepatic fibrosis markers, positioning tesamorelin as a candidate for metabolic liver disease intervention.
Synthesis Overview
Tesamorelin is synthesized via Fmoc solid-phase peptide synthesis, incorporating the full 44-amino acid GHRH sequence with an N-terminal trans-3-hexenoic acid modification. This lipophilic modification enhances metabolic stability without significantly altering receptor binding. The synthesis requires careful attention to aggregation-prone sequences and pseudoproline dipeptide incorporation for difficult couplings. Post-synthesis, the peptide is purified via preparative HPLC and characterized by mass spectrometry, amino acid analysis, and HPLC purity assessment.
Research Applications
- Visceral adipose tissue reduction and body composition studies
- HIV-associated lipodystrophy research
- GHRH receptor activation and signal transduction analysis
- IGF-1 elevation and metabolic parameter research
- Hepatic fat content and NAFLD/NASH investigation
- Cardiovascular biomarker effects in GH-stimulating protocols
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