Tesamorelin

Overview

Tesamorelin is a synthetic analogue of human growth hormone releasing hormone, based on the full 44 amino acid GHRH sequence rather than the shortened 1-29 fragment used by CJC-1295 and related compounds. It carries a trans-3-hexenoyl group attached to the N-terminal tyrosine, a modification whose purpose is to slow enzymatic breakdown. It is the third best selling compound in our range. We supply it as a lyophilised powder at 5mg per vial with an independent batch certificate of analysis reporting HPLC purity and mass spectrometry identity.

Mechanism of Action

Native GHRH is cleaved rapidly at the N-terminus by dipeptidyl peptidase 4, which is the main route by which the signal is terminated. The hexenoyl modification on tesamorelin sterically blocks that cleavage site, extending the window over which the analogue remains intact in plasma while leaving the receptor-binding region unchanged. Ferdinandi and colleagues published the non-clinical pharmacology and safety evaluation of the compound under its development code TH9507 [1], which remains the clearest published description of its pharmacokinetic profile. Later transcriptomic work by Fourman and colleagues examined hepatic gene expression signatures under the analogue [2]. Because it acts at the GHRH receptor rather than at the ghrelin receptor, it belongs to a different mechanistic half of the growth hormone secretagogue category to Ipamorelin and GHRP-6. Not intended for human or veterinary use.

Research Effects

References

1. [1]Ferdinandi ES, Brazeau P, High K, et al.. Non-clinical pharmacology and safety evaluation of TH9507, a human growth hormone-releasing factor analogue. Basic Clin Pharmacol Toxicol. 2007. PMID 17214611 · doi:10.1111/j.1742-7843.2007.00008.x
2. [2]Fourman LT, Billingsley JM, Agyapong G, et al.. Effects of tesamorelin on hepatic transcriptomic signatures in HIV-associated NAFLD. JCI Insight. 2020. PMID 32701508 · doi:10.1172/jci.insight.140134

Cited for the molecular pathways described above. Listing a study is not a claim about any outcome in humans.