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Tesamorelin: Chemistry Profile & Research Overview

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Tesamorelin

CAS 901758-09-6 · C₂₂₁H₃₆₆N₇₂O₆₇S · 5,135.9 g/mol

What Is Tesamorelin?

Tesamorelin is a synthetic 44-amino-acid analog of growth hormone-releasing hormone (GHRH), assigned CAS number 901758-09-6. It is distinguished from native human GHRH(1-44) by a trans-3-hexenoic acid group attached at the N-terminus, a chemical modification that increases the molecule’s resistance to enzymatic degradation. ITide Labs supplies Tesamorelin as a reference compound for laboratory research conducted by qualified professionals.

Chemical Properties

Compound nameTesamorelin
SynonymsTH9507, Tesamorelin acetate (salt form)
CAS Number901758-09-6
Molecular FormulaC₂₂₁H₃₆₆N₇₂O₆₇S
Molecular Weight5,135.9 g/mol
Peptide length44 amino acids
FormWhite lyophilized powder
Storage2–8 °C, protected from light
PubChem CID16132436

Historical Development and Discovery

Tesamorelin was developed by Theratechnologies in the early 2000s as a stabilized analog of native GHRH. The compound was designed to address the very short serum half-life of unmodified GHRH(1-44), which is rapidly cleaved at its N-terminus by dipeptidyl peptidase-IV (DPP-IV).

The first detailed non-clinical pharmacology and safety characterization of the molecule (then designated TH9507) was published in 2007 by Ferdinandi and colleagues, which remains a foundational chemistry reference for the analog.

Chemical Architecture and Structural Features

Tesamorelin’s 44-amino-acid sequence mirrors that of native human GHRH. The defining structural feature is the addition of a trans-3-hexenoic acid moiety at the N-terminal tyrosine (position 1), which blocks the DPP-IV cleavage site between residues 2 and 3. The peptide is a single-chain molecule with no internal disulfide bridges and is supplied as the acetate salt for laboratory handling. The hydrophobic N-terminal modification also marginally increases overall hydrophobicity relative to unmodified GHRH, a property relevant for solid-phase synthesis and chromatographic characterization.

Research Mechanisms

In the published peer-reviewed literature, Tesamorelin is described as a full agonist at the growth hormone-releasing hormone receptor (GHRH-R), a class B G-protein-coupled receptor expressed in the anterior pituitary. The N-terminal hexenoic acid modification confers two chemistry-relevant properties that make Tesamorelin a useful research probe: resistance to DPP-IV cleavage, and improved binding affinity stability across pH conditions encountered in standard receptor binding assays. These properties are why Tesamorelin appears in the medicinal-chemistry literature as a reference compound for GHRH receptor agonism studies.

Research Areas

What Is a GHRH Analog?

A GHRH analog is a synthetic peptide that mimics the binding behavior of endogenous growth hormone-releasing hormone at the GHRH receptor. Analogs are designed by introducing chemical modifications — N-terminal acylation, amino acid substitution, or backbone constraint — to alter properties such as receptor selectivity, proteolytic stability, and physicochemical handling characteristics. Tesamorelin is among the most extensively characterized N-terminally modified GHRH analogs in the peer-reviewed literature.

GHRH Receptor Signaling Research

The GHRH receptor (GHRH-R) is a class B G-protein-coupled receptor that signals primarily through Gαs, producing intracellular cyclic AMP accumulation upon agonist binding. Tesamorelin is used as a reference agonist in cell-based receptor signaling assays — for example, cAMP accumulation assays in cells transfected with the human GHRH-R — because its potency and stability profile have been well characterized.

Stabilized Peptide Design

Tesamorelin’s N-terminal modification is a frequently cited example of a successful protease-stabilization strategy in peptide drug design. The compound appears in medicinal-chemistry reviews of peptide stabilization techniques alongside other approaches such as D-amino acid substitution, backbone N-methylation, and cyclization. Researchers studying analog design principles use Tesamorelin as a comparator molecule.

Quality Assurance

Every ITide Labs lot of Tesamorelin is third-party tested for purity by HPLC and Mass Spec, with the Certificate of Analysis published on the product page. Industry benchmark for research-grade peptides is ≥98% purity; ITide Labs targets 99%+.

Frequently Asked Questions

What is the CAS number for Tesamorelin?

Tesamorelin’s CAS Registry Number is 901758-09-6.

What is the amino acid sequence of Tesamorelin?

Tesamorelin has the same 44-amino-acid sequence as native human GHRH(1-44) — YADAIFTNSYRKVLGQLSARKLLQDIMSRQQGESNQERGARARL — with a trans-3-hexenoic acid group attached at the N-terminal tyrosine.

What is the molecular weight of Tesamorelin?

The free-base molecular weight is 5,135.9 g/mol; the empirical formula is C₂₂₁H₃₆₆N₇₂O₆₇S.

How does Tesamorelin differ from native GHRH?

The peptide backbone is identical, but Tesamorelin carries a trans-3-hexenoic acid modification at the N-terminus. This modification blocks the dipeptidyl peptidase-IV (DPP-IV) cleavage site at residues 2–3, giving Tesamorelin substantially longer serum stability than unmodified GHRH(1-44).

What is the N-terminal modification on Tesamorelin?

The modification is a trans-3-hexenoic acid group (a six-carbon unsaturated fatty acid) attached via an amide bond to the N-terminal tyrosine residue.

Why is Tesamorelin used in research?

Tesamorelin is used in the literature as a reference GHRH analog — in GHRH-R receptor binding and cAMP signaling assays, in medicinal-chemistry studies of peptide stabilization strategies, and as a comparator in pharmacology screens of synthetic GHRH analogs.

Is Tesamorelin a peptide or a small molecule?

Tesamorelin is a 44-amino-acid peptide (a stabilized analog of GHRH), not a small molecule.

What laboratory storage does Tesamorelin require?

The lyophilized powder is stored at 2–8 °C and protected from light. Specific laboratory handling and preparation procedures are determined by the research laboratory’s own validated procedures.

Who developed Tesamorelin?

Tesamorelin was developed by Theratechnologies (Montréal, Canada) in the early 2000s under the development code TH9507. Foundational chemistry and pharmacology data were published by Ferdinandi et al. in 2007.

Is Tesamorelin available in different sizes from ITide Labs?

Yes — Tesamorelin 5mg vials are available now. A 10mg presentation is launching soon; join the waitlist on the Tesamorelin product page to be notified when 10mg is released.

CitationFerdinandi ES, Brazeau P, High K, Procter B, Fennell S, Dubreuil P. Non-clinical pharmacology and safety evaluation of TH9507, a human growth hormone-releasing factor analogue. Basic & Clinical Pharmacology & Toxicology. 2007;100(1):49–58. PubMed: 17214608.

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