Key findings
- The first constituent is the 1-44 amide with a trans-3-hexenoyl group on Tyr1, a change that made it resistant to dipeptidyl aminopeptidase IV and slowed its degradation in rat, dog and human plasma. [1]
- The second constituent is the pentapeptide Aib-His-D-2-Nal-D-Phe-Lys-NH2, which released growth hormone from primary rat pituitary cells with an EC50 of 1.3 nmol/l. [2]
- Antagonist profiling put the pentapeptide response at a GHRP-like receptor rather than the growth hormone releasing hormone receptor, so the two constituents are characterised through different pathways. [2]
- Detection work lists the larger growth hormone releasing hormone analogues as separate analytes with their own in-vitro metabolites, so each constituent of a mixture has to be identified in its own right. [3]
Identity and structure
- Catalog name
- A two-component listing whose name gives neither constituent amount
- Composition
- Constituent amounts come from the lot documentation; this profile does not assign them, and a combined fill mass does not give the amount of either peptide
- First constituent
- A 44 amino acid analogue of human growth hormone releasing factor carrying a trans-3-hexenoyl group on Tyr1 [1]
- Second constituent
- The pentapeptide Aib-His-D-2-Nal-D-Phe-Lys-NH2 [2]
- Form as supplied
- Sterile lyophilized powder
Mechanism as studied
The two constituents reach growth hormone release by different receptors in the cited work. The growth hormone releasing factor analogue addresses the dipeptidyl peptidase IV cleavage that inactivates the native hormone, which kinetic work located between Ala2 and Asp3. [1][4]
Antagonist profiling in primary rat pituitary cells placed the pentapeptide at a GHRP-like receptor. The same study found no change in follicle stimulating hormone, luteinizing hormone, prolactin or thyroid stimulating hormone and no rise in adrenocorticotropic hormone or cortisol. [2]
Research findings
- System
- Rat, dog and human plasma for in-vitro degradation alongside repeat-exposure work in rats, dogs and pigs; the study material is the growth hormone releasing factor analogue alone
- Measured
- In-vitro degradation rate in each plasma, plasma elimination kinetics, growth hormone and insulin-like growth factor 1, apparent elimination half-life
- Reported
- The trans-3-hexenoyl modification slowed in-vitro degradation in rat, dog and human plasma and prolonged plasma elimination. Apparent elimination half-life in dogs ranged from 21 to 45 min. [1]
- System
- Primary rat pituitary cells with GHRP and growth hormone releasing hormone antagonists; the study material is the pentapeptide alone
- Measured
- Growth hormone release potency and efficacy relative to GHRP-6, receptor pathway by antagonist blockade
- Reported
- EC50 was 1.3 plus or minus 0.4 nmol/l with an efficacy of 85 plus or minus 5 percent of the GHRP-6 maximum, and antagonist profiling indicated a GHRP-like receptor. [2]
- System
- Fortified urine containing the larger growth hormone releasing hormone analogues and nineteen synthesized in-vitro metabolites as reference materials; the pentapeptide is not among the analytes
- Measured
- Identity of the in-vitro metabolites and limits of detection by liquid chromatography tandem mass spectrometry
- Reported
- Nineteen major in-vitro metabolites were identified, synthesized and characterized in house as reference materials. Limits of detection for the target peptides were generally 1 ng/ml or less. [3]
Handling for in-vitro work
- Storage
- Lyophilized material kept at minus 20 degrees C, dark and dry; reconstituted aliquots kept cold and used promptly
Open questions
- No cited study characterises this mixture, so its stability, the behaviour of the two peptides together in solution and the identity of each constituent in a supplied vial remain documentation questions.
- Which analytical report establishes the amount of each constituent, as opposed to a single combined fill mass and one headline purity figure, is the document that would let a mixture-specific profile be written.
Lot records
Check the record for the exact material you order. A published paper and a batch certificate answer different questions.
- RV-24-0022-1 ↗Tesamorelin/Ipamorelin Blend · 99.10% HPLC2026-09-16
References
- Ferdinandi ES, Brazeau P, High K, et al. Non-clinical pharmacology and safety evaluation of TH9507, a human growth hormone-releasing factor analogue. Basic & clinical pharmacology & toxicology. 2007.
- Raun K, Hansen BS, Johansen NL, et al. Ipamorelin, the first selective growth hormone secretagogue. European journal of endocrinology. 1998.
- Memdouh S, Gavrilović I, Ng K, et al. Advances in the detection of growth hormone releasing hormone synthetic analogs. Drug testing and analysis. 2021.
- Bongers J, Lambros T, Ahmad M, et al. Kinetics of dipeptidyl peptidase IV proteolysis of growth hormone-releasing factor and analogs. Biochimica et biophysica acta. 1992.
Publication records fetched from PubMed on 2026-09-20. Profile text reviewed 2026-09-20.