Capromorelin Overview
Capromorelin (CP-424,391) is a nonpeptide, orally active small-molecule ghrelin receptor agonist and growth hormone secretagogue (GHS). It was originally developed by Pfizer as a candidate compound for the treatment of musculoskeletal frailty in elderly adults; those human clinical investigations were discontinued, and capromorelin was subsequently developed for veterinary use. Capromorelin (as the tartrate salt) is FDA-approved as Entyce (Elanco; dogs, 2016) and Elura (Elanco; cats with chronic kidney disease, 2020).
Kimera Chems supplies capromorelin as a research reagent for in vitro and analytical laboratory work, including GHS-R1a receptor pharmacology, analytical method development, and reference-standard applications. This product is not an FDA-approved veterinary or human drug formulation and is not intended for therapeutic substitution of Entyce, Elura, or any other prescription product.
Mechanism of Action
Capromorelin binds the growth hormone secretagogue receptor type 1a (GHS-R1a) and acts as a ghrelin mimetic. In published assays, capromorelin has been characterized with:
- hGHS-R1a binding affinity: K_i ≈ 7 nM
- Functional activity in rat pituicyte models: EC₅₀ ≈ 3 nM
- Oral bioavailability reported at approximately 65% (rat) and 44% (dog)
- Hepatic metabolism with renal excretion in published ADME studies
These receptor pharmacology and PK characteristics have supported capromorelin’s use as a reference GHS-R1a ligand in laboratory research.
Chemical Structure
- Chemical Name: 2-Amino-N-[(1R)-2-[(3aR)-3a-benzyl-2-methyl-3-oxo-2,3,3a,4,6,7-hexahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]-1-(benzyloxymethyl)-2-oxoethyl]-2-methylpropanamide
- Synonyms: CP-424,391; RQ-00000005
- CAS Number (free base): 193273-66-4
- CAS Number (tartrate salt): 193273-69-7
- Molecular Formula (free base): C₂₈H₃₅N₅O₄
- Molecular Weight (free base): 505.62 g/mol
- PubChem CID: 18000481
Structural identification and molecular data are referenced against PubChem and Merck Index records.
Product Format
- Form supplied: 10 mg powdered capsule
- Use: In vitro receptor pharmacology, analytical method development, and reference-standard laboratory work
Research Focus Areas
Capromorelin is commonly referenced in laboratory research involving:
- GHS-R1a binding and signaling pathway studies
- Ghrelin receptor pharmacology and structure-activity relationship analysis
- Analytical and reference-standard work (capromorelin is included in published LC-MS/MS panels for ghrelin receptor agonist detection)
- In vitro metabolism and ADME studies
- Comparative GHS pharmacology research alongside related ghrelin receptor ligands
Handling & Storage
- Store in a cool, dry location, protected from light
- Recommended long-term storage at -20 °C
- Keep tightly sealed when not in use
- Use appropriate laboratory handling procedures and PPE
Important Research Disclaimer
Capromorelin is supplied by Kimera Chems strictly as a research reagent for laboratory use only (RUO). This product is not intended for human consumption, off-label veterinary use, therapeutic substitution of FDA-approved veterinary products (Entyce, Elura), diagnostic application, or any other clinical purpose. All handling and use must comply with applicable federal, state, and local laws and institutional laboratory safety standards. Customers must accept Kimera Chems’ Terms and Conditions before ordering.
| CAS Number | 193273-69-7 |
| Other Names | 2-Amino-N-[(1R)-2-[(3aR)-2,3,3a,4,6,7-hexahydro-2-methyl-3-oxo-3a-(phenylmethyl)-5H-pyrazolo[4,3-c]pyridin-5-yl]-2-oxo-1-propanamide (2R,3R)-2,3-dihydroxybutanedioate, CP 424391-18, CP-424391 tartrate |
| IUPAC Name | N-[(2R)-1-[(3aR)-3a-benzyl-2-methyl-3-oxo-6,7-dihydro-4H-pyrazolo[4,3-c]pyridin-5-yl]-1-oxo-3-phenylmethoxypropan-2-yl]-2-amino-2-methylpropanamide;(2R,3R)-2,3-dihydroxybutanedioic acid |
| Molecular Formula | C₂₈H₃₅N₅O₄ |
| Molecular Weight | 505.62 |
| Dry-Fill Capsule Concentration | 10mg |
| Liquid Concentration And Solution | 20mg/ml PEG400, DMSO |
