Tesamorelin, developed under the research code TH9507, is a synthetic 44-residue amidated analog of human growth-hormone-releasing hormone, GHRH(1-44)-NH2, modified by acylation of the N-terminal tyrosine with a trans-3-hexenoyl group. Apart from that single non-natural N-terminal cap the sequence is the full-length native hormone, which distinguishes it from the truncated GRF(1-29) analogs.

Reported pharmacology places it as an agonist at the class B G-protein-coupled GHRH receptor (GHRHR), a Gs-coupled receptor for which activated cryo-EM structures have been described. In plasma incubation experiments the hexenoyl cap is reported to slow cleavage of the peptide by dipeptidyl aminopeptidase-IV relative to unmodified GHRH(1-44)-NH2.

Cited in GPCR structural biology and receptor pharmacology, peptide-stability and in-vitro metabolite characterisation, pituitary cell models and LC-MS/MS analytical method development. Supplied as a lyophilized solid.

Research use only. This material is sold for in-vitro laboratory research and development purposes exclusively. It is not a drug, food, or dietary supplement, has not been evaluated by the FDA, and must not be used in humans or animals.