Capromorelin

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.

Physical & Handling Properties

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.

Frequently Asked Research Questions

How does Capromorelin differ from peptide-based growth hormone secretagogues?

Unlike peptide-based agents, Capromorelin is a nonpeptide pyrazolo-piperidine small molecule. This structural difference provides it with distinct chemical stability, lipophilicity, and pharmacokinetic characteristics, making it an excellent comparative standard for studying ligand-receptor interactions.

What are the primary binding parameters of Capromorelin at the GHS-R1a receptor?

In published pharmacodynamic models, Capromorelin exhibits a highly potent binding affinity (Kᵢ ≈ 7 nM) for the human growth hormone secretagogue receptor GHS-R1a and drives functional intracellular activity with an EC₅₀ of approximately 3 nM in pituitary models.

Scientific References

1. Carpino, P. A., Lefker, B. A., Toler, S. M., Pan, L. C., Hadcock, J. R., Murray, M. C., et al. (2002). "Discovery and biological characterization of capromorelin analogues with extended half-lives." Bioorganic & Medicinal Chemistry Letters, 12(22), 3279–3282. doi:10.1016/s0960-894x(02)00734-5.

2. Khojasteh-Bakht, S. C., O'Donnell, P. J., Fouda, H. G., & Potchoiba, M. J. (2005). "Metabolism, pharmacokinetics, tissue distribution, and excretion of [14C]CP-424391 in rats." Drug Metabolism and Disposition, 33(1), 190–199. doi:10.1124/dmd.104.001065.

3. Rhodes, L., Zollers, B., Wofford, J. A., & Heinen, E. (2018). "Capromorelin: a ghrelin receptor agonist and novel therapy for stimulation of appetite in dogs." Journal of Veterinary Pharmacology and Therapeutics, 41(2), 167–176. doi:10.1111/jvp.12411.

Meta Description

Capromorelin (CAS 193273-66-4) is a ghrelin receptor agonist and GHS-R1a ligand for in vitro pharmacology assays. RUO.

Research Use Only Disclaimer: This product is labeled and sold "For Research Use Only - NOT FOR HUMAN CONSUMPTION." It is not a drug, dietary supplement, food, cosmetic, or medical device, and it is not approved by the FDA or any other regulator for human or veterinary use. It is supplied to approved account holders as a research chemical for laboratory use and must be handled in accordance with applicable law.