Ipamorelin / Tesamorelin Blend

This blend pairs two peptides with different receptor targets. Ipamorelin is the pentapeptide Aib-His-D-2-Nal-D-Phe-Lys-NH2, which acts at the ghrelin receptor. Tesamorelin, developed under the code TH9507, is an analog of the 44-residue growth hormone-releasing factor amide, minimally modified by attaching a trans-3-hexenoyl group to Tyr1; that modification makes the peptide resistant to deactivation by dipeptidyl aminopeptidase-IV. The two components therefore address the ghrelin receptor and the GHRH receptor respectively.

Ipamorelin / Tesamorelin Blend in the research literature

Ipamorelin released growth hormone from primary rat pituitary cells with potency and efficacy similar to GHRP-6, and antagonist profiling placed its action at a GHRP-type receptor rather than the GHRH receptor; in swine it did not alter FSH, LH, prolactin or TSH, and unlike GHRP-6 and GHRP-2 it did not raise ACTH or cortisol above levels seen with GHRH stimulation.

Animal pharmacology work on TH9507 reported that the hexenoyl modification slowed in vitro degradation of the peptide in rat and dog plasma relative to the unmodified releasing factor and prolonged plasma elimination kinetics of immunoreactive material, with apparent elimination half-life in dogs of 21 to 45 minutes. Plasma growth hormone and IGF-1 rose in pigs, rats and dogs.