Capromorelin

Capromorelin (CP-424,391) is a nonpeptide, orally active small-molecule ghrelin receptor agonist and growth hormone secretagogue (GHS). Originally developed to investigate musculoskeletal frailty in clinical models, this compound acts as a selective ghrelin mimetic by targeting the growth hormone secretagogue receptor type 1a (GHS-R1a). Capromorelin serves as a highly valuable reference ligand in neurochemistry, endocrinology, and analytical method-development settings, offering researchers a precise tool for exploring GHS-R1a binding dynamics, growth hormone stimulation, and downstream metabolic cascades.

Technical Specifications

Research Applications & Mechanism of Interest

In biochemical and molecular assays, Capromorelin functions as a selective mimetic of endogenous ghrelin, specifically binding the G-protein coupled GHS-R1a receptor to trigger intracellular signaling pathways. Research published in Bioorganic & Medicinal Chemistry Letters characterizes Capromorelin with a high-affinity GHS-R1a binding profile (Kᵢ ≈ 7 nM) and robust functional activity in pituitary models (EC₅₀ ≈ 3 nM).

Kimera Chems provides this compound to support rigorous in vitro and analytical investigation. Key laboratory focus areas include:

• GHS-R1a Binding & Signaling Kinetics: Investigating ligand-receptor docking configurations, second-messenger cascade activation (such as intracellular calcium mobilization), and receptor internalization profiles.

• Structure-Activity Relationships (SAR): Evaluating how the specific pyrazolinone-piperidine architecture of Capromorelin influences binding affinity and selectivity compared to endogenous ghrelin or peptide-based growth hormone secretagogues.

• Analytical Method Validation: Serving as a crucial reference standard for the development and calibration of high-resolution liquid chromatography-mass spectrometry (LC-MS/MS) screening panels designed to detect ghrelin receptor agonists.

• In Vitro ADME & Metabolic Profiling: Mapping enzyme-mediated degradative pathways, hepatic clearance rates, and metabolite profiles using isolated cellular matrices.

Storage & Handling Guidelines

Store at controlled room temperature. Keep tightly closed. Liquid formats: do not refrigerate or freeze. Cold storage may cause the solution to cloud or precipitate. If this occurs, return to room temperature and mix until clear.

Storage guidance is a house recommendation. Analytical documentation is per-lot release testing.