Tesamorelin is a synthetic analogue of growth hormone-releasing hormone (GHRH) that takes a different route to stability from most of its relatives. Rather than shortening the peptide and substituting amino acids, it retains the full 44-residue human GHRH sequence and adds a single acyl group at the N-terminus. It is also unusual among the peptides discussed in this cluster in having been approved as a medicine in one jurisdiction. This article explains its structure, its regulatory background and how it compares with other GHRH analogues.
For laboratory research use only. Not for human or veterinary use. See our research use only policy.
For an overview of GHRH analogues and the GHRP class, see our pillar guide to CJC-1295 and ipamorelin in research.
At a glance: tesamorelin
- Name: Tesamorelin
- Synonyms: TH9507, N-(trans-3-hexenoyl)-hGHRH(1-44)-NH2
- Sequence: trans-3-hexenoyl-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
- Molecular formula: C221H366N72O67S
- Molecular weight: 5135.9 g/mol
- CAS number: 218949-48-5
- Form: Lyophilised powder
- Purity: >99% (HPLC)
- Storage: 2-8°C, dark, upright, do not freeze. Keep sealed until use.
Background: native GHRH
Human GHRH was isolated and sequenced in 1982 by two groups, led by Roger Guillemin and by Jean Rivier and Wylie Vale, from pancreatic tumours that had caused acromegaly. The mature hypothalamic peptide is a 44-amino-acid C-terminal amide. It is released into the hypophyseal portal circulation and acts at the GHRH receptor, a class B G protein-coupled receptor on pituitary somatotrophs, to stimulate growth hormone synthesis and release.
Native GHRH is short-lived in plasma. The principal route of inactivation is cleavage by dipeptidyl peptidase-4 (DPP-4), which removes the N-terminal Tyr-Ala dipeptide to leave GHRH(3-44), a fragment with greatly reduced activity at the receptor. Most stabilised analogues are designed to protect this N-terminal site.
How tesamorelin is stabilised
Tesamorelin addresses the DPP-4 problem by attaching a trans-3-hexenoyl group, a six-carbon unsaturated acyl chain, to the alpha-amino group of the N-terminal tyrosine. DPP-4 requires a free N-terminal amine to recognise its substrates, so capping the amine with an acyl group hinders this cleavage. The remainder of the molecule is the unaltered human sequence, including methionine at position 27.
This contrasts with the approach used in modified GRF (1-29), also called CJC-1295 no DAC, which keeps only the first 29 residues and introduces four amino acid substitutions, including D-alanine at position 2. It also differs from CJC-1295 with DAC, which adds an albumin-binding maleimide group to extend circulating half-life to several days.
Comparing the three GHRH approaches
- Tesamorelin: full 44 residues, native sequence, N-terminal trans-3-hexenoyl cap.
- CJC-1295 no DAC: 29 residues, four substitutions (D-Ala2, Gln8, Ala15, Leu27), C-terminal amide.
- CJC-1295 with DAC: the same 29-residue backbone plus a lysine carrying a maleimidopropionyl group for covalent albumin binding.
Practical considerations of a larger peptide
At 5135.9 g/mol, tesamorelin is the largest peptide in this cluster, and the presence of methionine means it retains an oxidation-prone residue that Mod GRF 1-29 removes. For analytical work, this makes it relevant to monitor for oxidised species alongside the main peak when interpreting HPLC and mass spectrometry data. Our article on reading a peptide certificate of analysis explains how these techniques are used to confirm identity and purity.
Regulatory history
Tesamorelin was developed by the Canadian company Theratechnologies under the code TH9507. Clinical development culminated in phase 3 trials, one of which was published by Falutz and colleagues in the New England Journal of Medicine in 2007. In November 2010 the US Food and Drug Administration approved a tesamorelin product for a specific indication relating to abdominal fat accumulation associated with lipodystrophy in adults living with HIV.
This regulatory fact is stated for context only. The tesamorelin listed by Compound Cave is not a medicine, is not the approved product and has not been assessed by any medicines regulator. It is supplied as a laboratory reagent for in vitro and research use.
Tesamorelin in the research literature
Beyond the registration trials, tesamorelin has been investigated as a tool for studying the GHRH receptor and the downstream growth hormone and IGF-1 axis. Because its sequence is identical to the endogenous hormone apart from the N-terminal cap, it has been regarded as a close structural mimic of native GHRH with extended stability, which is useful when the aim is to model physiological ligand behaviour rather than that of a truncated fragment.
Like other GHRH receptor agonists, tesamorelin is often discussed alongside growth hormone-releasing peptides such as ipamorelin, which act at the separate ghrelin receptor. Researchers interested in other hypothalamic signalling peptides may also find our guide to kisspeptin-10 relevant, as it covers the reproductive axis rather than the somatotroph axis.
Storage and handling
Tesamorelin is supplied as a lyophilised powder in a sealed vial. We recommend storage at 2-8°C, away from light, kept upright and not frozen, and keeping the vial sealed until use. General guidance is covered in our article on how to store lyophilised peptides.
View tesamorelin in the catalogue.
Frequently asked questions
What is tesamorelin?
Tesamorelin is a synthetic analogue of human growth hormone-releasing hormone. It consists of the full 44-amino-acid human GHRH sequence with a trans-3-hexenoyl group attached to the N-terminal tyrosine, which stabilises the peptide against enzymatic cleavage.
How does tesamorelin differ from CJC-1295 no DAC?
CJC-1295 no DAC is a 29-residue fragment stabilised by four amino acid substitutions. Tesamorelin keeps the full 44-residue native sequence unchanged and is stabilised instead by a single acyl group at the N-terminus.
Is tesamorelin an approved medicine?
A tesamorelin product was approved by the US Food and Drug Administration in 2010 for a specific indication in adults living with HIV. The material sold by Compound Cave is not a medicine, is not that product and is supplied only for laboratory research.
Why is there no sequence listed as a short code?
Tesamorelin is the native 44-residue human GHRH amide with an N-terminal modification, so it is usually described as N-(trans-3-hexenoyl)-hGHRH(1-44)-NH2 rather than written out as a modified sequence.
How should lyophilised tesamorelin be stored?
We recommend storage at 2-8°C, in the dark, upright and not frozen, with the vial kept sealed until use.
References
- 1. Guillemin R, Brazeau P, Böhlen P, et al. Growth hormone-releasing factor from a human pancreatic tumor that caused acromegaly. Science. 1982;218:585-587.
- 2. Rivier J, Spiess J, Thorner M, Vale W. Characterization of a growth hormone-releasing factor from a human pancreatic islet tumour. Nature. 1982;300:276-278.
- 3. Falutz J, Allas S, Blot K, et al. Metabolic effects of a growth hormone-releasing factor in patients with HIV. N Engl J Med. 2007;357:2359-2370.
For laboratory research use only. Not for human or veterinary use. See our research use only policy.