Ac-[Tyr1,D-Phe2]-GRF (1-29) amide (human) CAS NO.93965-89-0

TECHNICAL SPECIFICATIONS

1.MECHANISM OF ACTION

This analog functions as a potent and selective agonist for the Growth Hormone-Releasing Hormone Receptor (GHRHR). The modifications (Acetyl-Tyr1, D-Phe2) dramatically increase its stability against plasma degradation, particularly from DPP-IV, which normally cleaves the native peptide after position 2 (Ala2). This allows it to reach and activate pituitary GHRHR more effectively. Upon binding to this Gs-protein coupled receptor, it stimulates adenylate cyclase, leading to a sustained increase in intracellular cyclic AMP (cAMP).

2.PRODUCT INDICATIONS

• Stable GHRH Agonist Studies: Investigating prolonged GH secretion dynamics in vitroand in vivodue to its enhanced pharmacokinetic profile compared to native GHRH.

• Receptor Signaling & Trafficking: Studying sustained cAMP-mediated signaling and GHRHR internalization using a degradation-resistant ligand.

• Animal Models of GH Deficiency: Administering to laboratory animals as a reliable and potent stimulator of GH for research on growth, metabolism, and aging.

• Drug Discovery & Comparative Pharmacology: Serving as a benchmark compound for evaluating the potency and stability of novel GHRH analogs or growth hormone secretagogues.

• In VitroPituitary Cell Assays: Using primary pituitary cell cultures or somatotroph cell lines to study GH synthesis and secretion with minimal peptide degradation interference.

• Structure-Activity Relationship (SAR) Research: Illustrating the impact of N-terminal modifications (acetylation, D-amino acid substitution) on peptide stability and bioactivity.

3.CLINICAL EFFICACY OF PRODUCT

• Research & Preclinical Efficacy: It is a highly effective stimulator of GH release in animal models, with potency and duration of action superior to native GHRH(1-29) due to its stability.

• Clinical Analogs: This compound belongs to a class of stabilized GHRH analogs that have been developed for clinical use. Tesamorelin (Egrifta®), an analog with similar stabilizing modifications (including a D-amino acid at position 2), is FDA-approved for treating HIV-associated lipodystrophy.

• Diagnostic Use: Analogs in this class have been used in diagnostic GH stimulation tests (e.g., GHRH + arginine test) to assess pituitary function.

• Therapeutic Potential: Research with this analog supports the therapeutic concept of using stable GHRH analogs to safely elevate GH levels for conditions like growth hormone deficiency, aging-related frailty, and metabolic disorders, though this specific molecule is not a marketed drug.




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