CJC-1295 with DAC 5mg· 5mg

CJC-1295 with DAC binds the GHRH receptor, a class B G-protein coupled receptor expressed on pituitary somatotrophs. Receptor engagement activates Gas, elevates intracellular cAMP, and stimulates pulsatile growth hormone release. Unlike the native hormone, which is rapidly degraded by dipeptidyl peptidase-4 and other proteases, the modified peptide is resistant to proteolytic cleavage at the N-terminus due to the D-Ala substitution and other backbone modifications.

The DAC moiety at the C-terminus forms a covalent thioether bond with the free thiol of cysteine-34 on circulating serum albumin, generating an albumin-peptide conjugate that escapes renal filtration and proteolytic clearance. This produces sustained low-level GHRH receptor activation rather than the pulsatile pattern observed with short-acting analogs. The pharmacodynamic consequence is a sustained, modest elevation in growth hormone and IGF-1 levels, in contrast to the high-amplitude pulses generated by shorter-acting GHRH peptides.