Hexarelin — wholesale 10-vial kits

Research context

Hexarelin differs from GHRP-6 by a single methyl group on the D-tryptophan at position 2. The substitution was introduced because 2-methyl-tryptophan is chemically more stable than tryptophan. In the first rat studies (Deghenghi et al., Life Sciences, 1994) hexarelin was a highly effective GH releaser, matching GHRP-6 by the intravenous route and producing longer-lasting, slightly greater release in a second paradigm. Human endocrine studies describe it as a potent GHRP whose GH response is larger than that to GHRH and additive with it, and which is abolished by somatostatin (Arvat et al., Neuroendocrinology, 1995).

Hexarelin and the discovery of CD36 as a GHRP binding site. Hexarelin is the molecule through which the GHRP family's second receptor was found. Perfused-heart experiments showed a coronary response to hexarelin, and a photoactivatable radiolabelled hexarelin derivative labelled an 84-kDa binding site in rat cardiac membranes that the non-peptide secretagogues MK-0677 and EP51389 did not displace, neither of which reproduced the coronary effect (Bodart et al., 1999). N-terminal sequencing of the deglycosylated protein identified it as CD36, and the response was absent in hearts from CD36-null mice and from CD36-deficient rats (Bodart et al., 2002). Photoaffinity cross-linking later mapped hexarelin's binding site to CD36 residues Asn132–Glu177, overlapping the oxidized-LDL binding region, with Met169 as the apparent contact point (Demers et al., Biochemical Journal, 2004).

Much of hexarelin's research use follows from that split: cardiac-tissue studies use it to probe CD36-mediated signaling independent of growth-hormone release, while endocrine studies use it to examine desensitization of the GHS-R1a response with repeated exposure, which published work in healthy elderly volunteers describes as partial and reversible, with the GH response returning to baseline four weeks after a 16-week period of repeated exposure (Rahim and Shalet, 1998).

U.S. regulatory status: hexarelin is not an FDA-approved drug and has never been marketed as one. WholesalePeptide.us supplies it only for in-vitro, analytical and preclinical laboratory research.

Because hexarelin and GHRP-6 differ by only a methyl group (14 Da), LC-MS identity on the COA is the simplest way to confirm which peptide is in a vial; the two co-elute closely on many RP-HPLC methods. Every lot we sell carries a lot-specific COA with both the chromatogram and the measured mass, published before the lot ships. Hexarelin is often ordered together with GHRP-6 for side-by-side receptor and CD36-binding studies.

In the literature hexarelin is sometimes listed under its international nonproprietary name, examorelin, and searches for either name return the same body of work. Groups extending the CD36 line usually hold hexarelin as the reference ligand while testing azapeptide analogs derived from GHRP-6, since the two peptides are what the original binding and knockout experiments were built on. Hexarelin is a lyophilized single-compound kit with no blend partner in our catalog.

Research areas

• Ghrelin receptor (GHS-R1a) agonism and desensitization
• CD36 binding in cardiac models
• Photoaffinity mapping of CD36 ligand-binding domains
• Structure–activity comparisons with GHRP-6
• Pituitary cell models

U.S. regulatory status of the compound (as an active ingredient): Not approved by the FDA. The material sold here is a research reference chemical, not a drug product.

Handling and storage

• Store lyophilized vials at −20 °C, sealed, protected from light and moisture.
• Let the vial reach room temperature before opening to limit condensation on the powder.
• Reconstitute in a sterile buffer appropriate to the assay, following your lab's SOP.
• Aliquot reconstituted material and freeze once; avoid repeated freeze–thaw.