Description
Chemical Identity
Tesamorelin is a synthetic analog of human growth hormone-releasing hormone (GHRH) with the molecular formula C221H366N72O67S1 and a molecular weight of approximately 5135.9 Da. Consisting of 44 amino acids with a trans-3-hexenoic acid group attached to the N-terminal tyrosine residue, Tesamorelin was developed by Theratechnologies Inc. as a stabilized GHRH analog with enhanced resistance to enzymatic degradation by dipeptidyl peptidase-IV (DPP-IV).
Tesamorelin is also known by the following designations: Egrifta, Tesamorelin Acetate, TH9507.
| Property | Value |
|---|---|
| Molecular Formula | C221H366N72O67S1 |
| Molecular Weight | 5135.9 Da |
| CAS Number | 218949-48-5 |
| 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-Met-Ser-Arg-Gln-Gln-Gly-Glu-Ser-Asn-Gln-Glu-Arg-Gly-Ala-Arg-Ala-Arg-Leu-NH2 |
| Research Status | FDA Approved |
Research Overview
Tesamorelin has been investigated in Phase 3 clinical trials and post-marketing studies spanning metabolic, hepatic, and cognitive research domains. The primary mechanism of action involves activation of the GHRH receptor (GHRHR) on anterior pituitary somatotroph cells, stimulating physiological pulsatile growth hormone (GH) release while preserving normal feedback mechanisms through IGF-1 and somatostatin.
Key areas of published research include:
- Visceral Adipose Tissue Reduction: Two pivotal Phase 3 trials enrolling over 800 HIV-infected patients demonstrated significant visceral adipose tissue (VAT) reduction with Tesamorelin. The first pivotal trial showed a mean trunk fat reduction of 15.2% versus a 5.0% increase with placebo. The second trial confirmed approximately 14% VAT reduction from baseline, with treatment effects evident by week 13 and maintained through week 26.
- Hepatic Steatosis: The GILT trial, a randomized double-blind placebo-controlled study, demonstrated that Tesamorelin reduced hepatic fat fraction by 37% relative change from baseline versus 10% with placebo. Resolution of hepatic steatosis was achieved in 35% of treated subjects versus 4% with placebo, with improvements in NAFLD activity scores.
- Cognitive Function: A preliminary randomized trial in healthy older adults demonstrated improvements in executive function and verbal memory following Tesamorelin treatment over 20 weeks, with cognitive improvements correlating with IGF-1 increases.
Tesamorelin received FDA approval in November 2010 for the reduction of excess abdominal fat in HIV-infected patients with lipodystrophy. It remains the only FDA-approved treatment specifically indicated for this condition. The hepatic and cognitive indications remain investigational.
Specifications
All Tesamorelin supplied by Prescott Bio Canada is manufactured to research-grade standards.
| Specification | Detail |
|---|---|
| Purity | >98% (HPLC) |
| Form | Lyophilized powder |
| Appearance | White to off-white powder |
| Storage (lyophilized) | -20°C, protected from light |
| Storage (reconstituted) | 2-8°C, use within 30 days |
| Solubility | Soluble in bacteriostatic water, sterile water, or normal saline |
Each vial is accompanied by a Certificate of Analysis (COA) documenting purity, identity, and endotoxin testing.
Research Applications
Tesamorelin is supplied exclusively for in vitro and in vivo laboratory research. Published experimental applications include:
- Investigation of GHRH receptor-mediated growth hormone secretion and pulsatility patterns
- Assessment of visceral adipose tissue metabolism and lipolytic signaling pathways
- Study of hepatic lipid metabolism and de novo lipogenesis regulation
- Evaluation of GH/IGF-1 axis effects on cognitive function in aging models
Researchers should consult the primary literature and institutional review protocols before designing experiments with Tesamorelin.
Storage and Handling
Lyophilized powder: Store at -20°C in the original sealed vial, protected from light and moisture. Under these conditions, Tesamorelin maintains stability for up to 24 months.
Reconstituted solution: Reconstitute with bacteriostatic water or sterile water to the desired concentration. Store reconstituted Tesamorelin at 2-8°C and use within 30 days. Avoid repeated freeze-thaw cycles.
Handling precautions: This product is intended for research use only (RUO). Not for human or veterinary diagnostic or therapeutic use. Handle using standard laboratory safety practices including appropriate PPE.