Tesamorelina

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Precio por envase (10 viales). El descuento se aplica únicamente a este compuesto; no se admiten combinaciones.

Tesamorelin — Stabilized GHRH(1-44) Analogue with FDA-Approved Clinical Precedent

Tesamorelin (development code TH9507; brand name Egrifta) is a chemically stabilized analogue of endogenous growth hormone-releasing hormone consisting of the full 44-amino acid GHRH sequence conjugated at its N-terminus to a trans-3-hexenoic acid moiety. The modification was designed specifically to resist cleavage by dipeptidyl peptidase IV (DPP-IV), the enzyme responsible for the rapid inactivation of native GHRH in plasma. Tesamorelin received FDA approval in November 2010 for reduction of excess abdominal fat in HIV-infected patients with lipodystrophy — one of the few GHRH analogues to reach regulatory approval with Phase III data on a specific adiposity endpoint. This clinical history gives tesamorelin one of the most thoroughly documented pharmacokinetic and pharmacodynamic profiles among synthetic GHRH analogues available for research. Its mechanism is fundamentally that of a GHRHR agonist operating through the same pulsatile GH release pathway as endogenous GHRH, but with extended plasma stability and a more consistent receptor occupancy profile than the shorter sermorelin fragment.

Why Tesamorelin’s N-Terminal Modification Matters

The trans-3-hexenoic acid group conjugated to the N-terminus of GHRH(1-44) sterically blocks DPP-IV from cleaving the His-Ala bond at positions 1-2, which is the primary degradation site for native GHRH in vivo. The result is a 2–3-fold extension in plasma half-life compared to unmodified GHRH, without altering the GHRHR binding conformation — confirmed by the full preservation of Gs-coupled cAMP signaling downstream. The full 44-residue sequence (vs. sermorelin’s 29-residue truncation) provides marginally greater receptor contact area, but the primary pharmacokinetic advantage over sermorelin is the DPP-IV resistance rather than sequence length.

Aplicaciones de investigación

Tesamorelin is used in studies examining:

• GHRH analogue stability — DPP-IV resistance and plasma half-life characterization
• Visceral fat reduction mechanisms downstream of GH axis stimulation
• HIV-associated lipodystrophy models and adipose tissue redistribution
• IGF-1 axis regulation under sustained GHRHR stimulation
• Comparative GHRH pharmacology (sermorelin vs. tesamorelin vs. CJC-1295)
• Triglyceride metabolism in GH-deficient and lipodystrophic models

Especificaciones

Reconstitución

Tesamorelin arrives as lyophilized powder and must be reconstituted with bacteriostatic water prior to use. Use the formula:

Total en mg ÷ Volumen añadido (mL) = Concentración (mg/mL)

Ejemplo: vial de 5 mg + 1 ml de agua BAC = solución de 5 mg/ml; vial de 10 mg + 2 ml de agua BAC = solución de 5 mg/ml

El péptido reconstituido debe conservarse a una temperatura de entre 2 y 8 °C y utilizarse en un plazo de 28 a 30 días.

Notas sobre el protocolo

Tesamorelin’s research frameworks are anchored to its FDA-approved clinical protocol and the Phase III data underlying it. The approved regimen provides a well-characterized reference point for research designs examining the GHRH axis under sustained GHRHR stimulation.

• Dose range (clinical literature): 2mg SC once daily (FDA-approved protocol for HIV lipodystrophy)
• Frequency: Once daily in all Phase II and Phase III literature
• Study duration: 26–52 weeks in Phase III trials; shorter 8–12 week windows used in mechanistic GH axis studies

Pilas de investigación

Tesamorelin is commonly paired in research settings with:

• CJC-1295 No DAC — CJC-1295 No DAC is a GHRH analogue with overlapping receptor targets but distinct half-life kinetics; researchers pair both with Tesamorelin to compare pituitary GH pulse responses to full-length versus truncated GHRH analogues at matched receptor sites.
• Ipamorelin — Ipamorelin activates the ghrelin receptor (GHS-R1a), a mechanism independent of Tesamorelin’s GHRH receptor engagement. The combination is used in studies examining whether dual-pathway GH secretagogue stimulation produces additive or synergistic GH pulse amplitude effects.
• Sermorelin — Sermorelin is a shorter GHRH analogue (first 29 amino acids); pairing with Tesamorelin allows structural and kinetic comparisons within the GHRH peptide class, including receptor binding duration, GH pulse characteristics, and downstream IGF-1 response in research models.

Garantía de pureza

Cada lote tiene una pureza ≥99 %. Si sometes tu compuesto a un análisis independiente y los resultados no coinciden, envíanos el certificado de análisis (COA) y te concederemos un vale de compra sin hacerte preguntas.