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Tesamorelin | CAS: 901758-09-6

CAS Number:
901758-09-6
Chemical Classification:
Research peptide

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Tesamorelin (CAS 901758-09-6) is a stabilized growth hormone-releasing hormone analogue used to probe pituitary GH axis dynamics without the broad receptor cross-reactivity seen in some older secretagogues. Stabilizing substitutions extend peptide integrity in serum-containing media, which matters when pulse-frequency experiments run over 24–48 hours. Endocrine research contexts range from isolated pituitary somatotroph cultures to whole-animal GH pulsatility recording, and the appropriate readout—IGF-1, GH burst amplitude, or GHRH-receptor internalization—varies by laboratory focus. Typical workflows include subcutaneous bolus studies in rodent models, perifused pituitary fragments with calcium imaging, and comparative assays against native GHRH(1-44). Material is documented by COA, LC-MS, HPLC, and NMR and is restricted to research applications.

CAS
901758-09-6
Molecular Formula
C221H366N72O67S
Molecular Weight
5135.9 g/mol
Purity
≥98%
Appearance
White lyophilized powder
Storage
Store at -20°C

Analytical Documentation

COA✓ Available
LC-MS✓ Available
HPLC✓ Available
NMR✓ Available

Research Inquiry

Overview

Tesamorelin is a synthetic 44-amino-acid peptide analog of growth hormone-releasing hormone (GHRH), also known as growth hormone-releasing factor, engineered with transposition of two amino acids relative to the native sequence to enhance stability in research applications. It binds the GHRH receptor on pituitary somatotrophs, triggering growth hormone synthesis and secretion in endocrine signaling studies. Tesamorelin has become a standard pharmacological probe for investigating hypothalamic-pituitary growth hormone axis dynamics, pulsatile GH release patterns, and downstream insulin-like growth factor-1 production in preclinical endocrinology research. Unlike small-molecule ghrelin mimetics, tesamorelin acts through classical Gs-coupled GHRH receptor signaling, enabling pathway-specific dissection of somatotroph function in vitro and in vivo experimental systems. Supplied at ≥98% purity (C221H366N72O67S; 5135.9 g/mol), this material supports controlled laboratory investigation under research-use-only conditions.

Mechanism of Action

Tesamorelin activates GHRH receptor on anterior pituitary somatotrophs, stimulating adenylyl cyclase and protein kinase A phosphorylation of transcription factors that upregulate GH1 gene expression and promote GH vesicle exocytosis. Elevated circulating GH in research models increases hepatic IGF-1 synthesis through JAK-STAT signaling in hepatocytes, expanding the endocrine cascade studied in growth axis experiments. Negative feedback via somatostatin from hypothalamic periventricular neurons and IGF-1 at the hypothalamus and pituitary modulates tesamorelin-driven GH pulses. Tesamorelin does not act at ghrelin receptor (GHS-R1a) or prolactin-releasing pathways at research-relevant concentrations. Its mechanism supports comparative studies with GHS-R agonists to separate GHRH-dependent from ghrelin-dependent GH secretagogue biology.

Receptor Binding & Signaling

Tesamorelin binds GHRH receptor (GHRHR), a class B GPCR expressed predominantly on pituitary somatotrophs, with high affinity and full agonism in cAMP accumulation assays. Minimal cross-reactivity with GLP-1R, secretin receptor, or unrelated peptide receptors is reported at standard research concentrations. Species differences between human and rodent GHRHR sequences affect potency translation in transgenic versus native animal models. Receptor desensitization and internalization after sustained exposure influence pulsatiles GH release patterns in long-duration infusion experiments.

Research Applications

Somatotroph secretion and pulse analysis

Perifused pituitary cells and anterior pituitary explants use tesamorelin to induce GH release while measuring pulse frequency and amplitude with automated blood sampling systems in research animals. Investigators compare tesamorelin with GHS-R agonists to map distinct secretagogue pathways. Calcium imaging of somatotrophs reveals GHRH receptor coupling dynamics. These platforms support endocrine physiology research on growth hormone pulsatility without therapeutic intent.

IGF-1 axis and hepatic signaling

Rodent studies measure serum IGF-1, IGFBP profiles, and hepatic STAT5 phosphorylation following tesamorelin administration under controlled research protocols. Liver-specific receptor knockouts help attribute IGF-1 changes to direct GH action. Tesamorelin enables time-course experiments on growth axis feedback loops involving somatostatin and IGF-1. Data inform computational models of endocrine feedback in growth research.

Lipid metabolism and adipose research

GH axis activation via tesamorelin is used in research exploring visceral adipose lipolysis, hepatic VLDL production, and substrate oxidation in animal models. Pairing with GH receptor antagonists isolates GH-mediated metabolic effects from direct GHRH receptor actions at the pituitary. Tesamorelin supports mechanistic studies on growth hormone and lipid cross-talk in endocrine-metabolic laboratories.

GHRH receptor pharmacology

Cell lines expressing human GHRHR validate tesamorelin potency for batch release testing via cAMP and ERK readouts. Structure-activity comparisons with native GHRH(1-44) and truncated analogs map sequence requirements for receptor activation. Antagonists such as acetyl-(D-Arg2)-GHRH(5-29)amide confirm target specificity. These assays emphasize receptor biochemistry in discovery research.

Molecular Information

Sequence & Chain Summary

44-amino-acid GHRH(1-44) analog with N-terminal modifications (stabilized sequence).

Modification Type

Sequence transposition at positions 1-2 (GHRH analog design); supplied as acetate salt.

Structural Notes

Tesamorelin adopts an alpha-helical conformation required for GHRH receptor N-terminal domain engagement, with mass confirmed by high-resolution LC-MS. SPPS synthesis yields product requiring preparative HPLC and identity verification by peptide mapping. The peptide is susceptible to oxidative degradation at methionine residues during improper storage. Circular dichroism in membrane mimics confirms helical integrity for structural studies. Batch-specific molecular characterization—including mass confirmation and purity profiling—is available through COA, LC-MS, HPLC, and NMR documentation supplied with Tesamorelin.

Molecular Formula
C221H366N72O67S
Molecular Weight
5135.9 g/mol
Purity Specification
≥98%

Experimental Notes

Stability

Lyophilized tesamorelin remains stable at −20°C for extended storage when protected from moisture. Reconstituted solutions show activity loss with repeated freeze-thaw and prolonged room temperature exposure. Store aliquots at −80°C if long-term working stock is required. Oxidizing environments accelerate methionine sulfoxide formation detectable by HPLC. Lyophilized Tesamorelin should be protected from repeated freeze-thaw cycles, moisture, and prolonged exposure to ambient light where applicable. Analytical integrity is best preserved when material is stored under the conditions specified on the certificate of analysis.

Storage Conditions

Store at -20°C. Tesamorelin is supplied as white lyophilized powder. For long-term archival storage in research inventories, maintain sealed containers with desiccant where recommended and document lot numbers for traceability across experimental runs.

Laboratory Handling

Reconstitute with sterile water or dilute acetic acid buffer per laboratory SOP. Avoid frothing during dissolution. Use promptly after reconstitution or aliquot for frozen storage. Label concentrations in nmol/mL for endocrine assay consistency. Reconstitute only with appropriate research-grade solvents compatible with your assay format. Allow vials to reach equilibrium before opening, work under clean bench conditions, and label all working solutions with concentration, date, and researcher ID per institutional SOPs.

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Frequently Asked Questions

Research-focused answers about Tesamorelin. For laboratory use only — not medical advice.

What is Tesamorelin used for in research?
Tesamorelin is supplied for laboratory research on GHRH receptor signaling, growth hormone axis physiology, and related endocrine studies. It is not intended for human or veterinary treatment, athletic enhancement, or compounding into administered products.
How does Tesamorelin work biologically?
Tesamorelin stimulates GHRH receptors on pituitary somatotrophs, increasing cAMP and triggering growth hormone synthesis and release in research models. Downstream IGF-1 production extends the experimental endocrine cascade studied in growth axis research.
What receptors does Tesamorelin interact with?
The primary target is the growth hormone-releasing hormone receptor (GHRHR) on anterior pituitary somatotrophs. Meaningful activation of ghrelin receptor or unrelated secretagogue receptors is not observed at standard research concentrations.
Is Tesamorelin stable at room temperature?
Lyophilized tesamorelin remains stable at −20°C for extended storage when protected from moisture. Reconstituted solutions show activity loss with repeated freeze-thaw and prolonged room temperature exposure. Store aliquots at −80°C if long-term working stock is required. Oxidizing environments accelerate methionine sulfoxide formation detectable by HPLC. For short-term laboratory workflows, minimize time at room temperature and return unused material to recommended storage promptly. Tesamorelin is not formulated for ambient long-term storage.
What is the recommended storage condition for Tesamorelin?
Store at -20°C. Store lyophilized material in a dedicated −20°C freezer, protect from moisture ingress, and avoid repeated temperature cycling. Reconstituted solutions should be aliquoted and frozen if not used within the validated window of your internal stability study.