Capromorelin (tartrate)

Capromorelin is a growth hormone (GH) secretagogue and an agonist of GH secretagogue receptor 1a (GHS-R1a), which is also known as the ghrelin receptor. It stimulates GH release from primary rat pituitary cells with an EC50 value of 3 nM. Capromorelin (0.3, 3, and 30 nM) stimulates intracellular calcium mobilization in primary rat pituitary cells. It increases rat serum GH levels (ED50 = 0.04 mg/kg, i.v.) and decreases dog serum insulin-like growth factor 1 (IGF-1) levels when administered orally at a dose of 1 mg/kg. Capromorelin (3.9 mg/kg, once per day for 28 days) increases rat body weight by 43.6% without affecting whole-body percentages of fat, lean mass, or bone content. It decreases infarct size in a rabbit model of ischemia-reperfusion injury induced by left coronary artery occlusion when administered at a dose of 25 mg/kg. Formulations containing capromorelin have been used in the treatment of weight loss in cats with chronic kidney disease and as an appetite stimulant in dogs.Formal Name: 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-[(phenylmethoxy)methyl]ethyl]-2-methyl-propanamide, (2R,3R)-2,3-dihydroxybutanedioate. CAS Number: 193273-69-7. Synonyms: CP 424,391-18, RQ-00000005. Molecular Formula: C28H35N5O4 . C4H6O6. Formula Weight: 655.7. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: Soluble, Ethanol: Soluble. SMILES: OC([C@H](O)[C@@H](O)C(O)=O)=O.CN(C1=O)N=C(CCN(C2)C([C@H](NC(C(C)(N)C)=O)COCC3=CC=CC=C3)=O)[C@]12CC4=CC=CC=C4. InChi Code: InChI=1S/C28H35N5O4.C4H6O6/c1-27(2,29)25(35)30-22(18-37-17-21-12-8-5-9-13-21)24(34)33-15-14-23-28(19-33,26(36)32(3)31-23)16-20-10-6-4-7-11-20,5-1(3(7)8)2(6)4(9)10/h4-13,22H,14-19,29H2,1-3H3,(H,30,35),1-2,5-6H,(H,7,8)(H,9,10)/t22-,28-,1-,2-/m11/s1. InChi Key: MJGRJCMGMFLOET-MYPSAZMDSA-N.