Tesamorelin

Description

Tesamorelin Research Peptide

Tesamorelin is a synthetic analog of growth hormone-releasing hormone (GHRH) designed for advanced endocrinological and metabolic research applications. This modified peptide incorporates a trans-3-hexenoic acid group at its N-terminus, conferring enhanced stability and bioactivity relative to native GHRH(1-44). Tesamorelin is supplied exclusively for in vitro and in vivo laboratory research and is not intended for human consumption or clinical application.

Molecular Profile

• Amino Acid Count: 44 amino acids (modified GHRH analog)
• Molecular Weight: Approximately 5135.93 Da
• Classification: Growth hormone-releasing hormone (GHRH) analog; growth hormone secretagogue
• CAS Number: 218949-48-5
• Modification: Trans-3-hexenoic acid conjugated to the N-terminal tyrosine residue
• Physical Appearance: White to off-white lyophilized powder
• Solubility: Soluble in sterile water and dilute acidic aqueous solutions

Mechanism of Action

Tesamorelin acts as a specific agonist of the GHRH receptor (GHRHR), a class B G-protein coupled receptor expressed predominantly on somatotroph cells of the anterior pituitary gland. Upon binding, tesamorelin activates the Gs-alpha subunit, stimulating adenylyl cyclase and elevating intracellular cAMP levels. This signaling cascade activates protein kinase A (PKA), which in turn promotes the transcription of the growth hormone (GH) gene and stimulates the exocytosis of GH-containing secretory granules.

The N-terminal trans-3-hexenoic acid modification protects tesamorelin from aminopeptidase-mediated degradation, a primary route of inactivation for native GHRH. This structural enhancement results in improved metabolic stability while preserving full receptor agonist activity. In preclinical models, tesamorelin administration has been shown to produce pulsatile GH release that maintains the physiological secretory pattern, in contrast to exogenous GH administration which bypasses the hypothalamic-pituitary feedback axis.

Downstream of GH release, research models demonstrate activation of the GH/insulin-like growth factor-1 (IGF-1) axis, with hepatic IGF-1 production serving as a primary mediator of anabolic and metabolic effects. In adipose tissue research models, GH signaling promotes lipolysis through activation of hormone-sensitive lipase (HSL) and suppression of lipoprotein lipase (LPL), resulting in mobilization of stored triglycerides for oxidative metabolism.

Research Applications

• GH-IGF-1 Axis Research: Study of pulsatile GH secretion dynamics, IGF-1 production, and feedback regulation of the somatotropic axis in animal models and primary pituitary cell cultures
• Adipose Tissue Metabolism: Investigation of GH-mediated lipolysis, visceral adipose tissue reduction, and adipokine profile changes in research models of lipodystrophy and metabolic syndrome
• Body Composition Research: Assessment of changes in lean body mass, fat mass distribution, and substrate utilization under GHRH stimulation in preclinical models
• Hepatic Metabolism Studies: Examination of IGF-1-mediated effects on hepatic lipid metabolism, glucose output, and protein synthesis in liver cell lines and perfused liver models
• Neuroendocrine Research: Study of hypothalamic-pituitary axis regulation, somatostatin-GHRH interplay, and circadian GH secretory patterns
• Aging and Somatopause Models: Investigation of age-related decline in GH pulsatility and the capacity of GHRH analogs to restore somatotroph function in aged rodent models

Available Formulations

Kai Bio Labs provides tesamorelin in lyophilized form at the following research quantities:

• 2 mg — suitable for in vitro pituitary cell stimulation assays and receptor binding studies
• 6 mg — appropriate for in vivo research protocols requiring multi-day dosing in animal models

Each vial is sealed under nitrogen atmosphere. Reconstitute with sterile water for injection or bacteriostatic water prior to experimental use.

Certificate of Analysis

• Purity: ≥98% by RP-HPLC
• Identity: Confirmed by ESI-MS and amino acid composition analysis
• Endotoxin: LAL assay confirms levels within acceptable research-grade limits (<1.0 EU/mg)
• Sterility: Manufactured under aseptic conditions with sterility testing per USP <71>
• Peptide Content: Determined by quantitative amino acid analysis and UV absorbance
• Water Content: Verified by Karl Fischer titration

A Certificate of Analysis accompanies each shipment and is available by lot number upon request.

Storage and Handling

• Lyophilized: Store at -20°C for maximum stability; 2–8°C acceptable for up to 30 days
• Reconstituted: Store at 2–8°C. Use within 21 days of reconstitution. Do not freeze reconstituted solution
• Shelf Life: 24 months from manufacture when stored at -20°C in original sealed packaging
• Light Sensitivity: Protect from prolonged light exposure
• Reconstitution: Inject solvent slowly along the vial wall. Allow to dissolve by gentle swirling — do not shake vigorously

References

1. Spooner LM, Olin JL. “Tesamorelin: A Growth Hormone-Releasing Factor Analogue.” Clinical Therapeutics. 2012;34(3):572-583. doi:10.1016/j.clinthera.2012.01.016
2. Stanley TL, Grinspoon SK. “Effects of growth hormone-releasing hormone on visceral fat, metabolic, and cardiovascular indices in human studies.” Growth Hormone & IGF Research. 2015;25(2):59-65. doi:10.1016/j.ghir.2014.12.005
3. Falutz J, Allas S, Blot K, et al. “Metabolic effects of a growth hormone-releasing factor in patients with HIV.” New England Journal of Medicine. 2007;357(23):2359-2370. doi:10.1056/NEJMoa072375
4. Ionescu M, Bhatt DL, Engelen MPKJ. “Effects of tesamorelin on body composition, visceral fat, and metabolic parameters.” Journal of Clinical Endocrinology & Metabolism. 2014;99(3):891-901.

This product is intended for laboratory research use only. It is not a drug, food, or cosmetic and should not be used for human or veterinary diagnostic or therapeutic purposes. Handling should be performed by qualified research personnel in accordance with applicable institutional guidelines.