Anamorelin

Anamorelin is a small molecule agonist of the growth hormone (GH) secretagogue receptor 1a (GHS-R1a) and a mimetic of ghrelin (Cay-15072, Cay-24458, Ki = 0.7 nM). It induces calcium mobilization in CHO cells expressing rat GHS-R1a in a concentration-dependent manner and GH release from rat pituitary cells (EC50 = 1.5 nM). In vivo, anamorelin stimulates GH release in sham and vagotomized rats in a dose-dependent manner. Anamorelin (3-30 mg/kg) also increases food intake in rats. Formulations containing anamorelin have been used to treat cancer anorexia and cachexia in patients with non-small cell lung cancer.Formal Name: (3R)-1-[(2R)-2-[(2-amino-2-methyl-1-oxopropyl)amino]-3-(1H-indol-3-yl)-1-oxopropyl]-3-(phenylmethyl)-1,2,2-trimethylhydrazide, 3-piperidinecarboxylic acid. CAS Number: 249921-19-5. Synonyms: RC-1291. Molecular Formula: C31H42N6O3. Formula Weight: 546.7. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 25 mg/ml, DMSO: 20 mg/ml, Ethanol: 30 mg/ml, Ethanol:PBS (pH 7.2) (1:4): 0.20 mg/ml. lambdamax: 219 nm. SMILES: O=C(N(C)N(C)C)[C@]1(CC2=CC=CC=C2)CN(C([C@H](NC(C(C)(N)C)=O)CC3=CNC4=C3C=CC=C4)=O)CCC1. InChi Code: InChI=1S/C31H42N6O3/c1-30(2,32)28(39)34-26(18-23-20-33-25-15-10-9-14-24(23)25)27(38)37-17-11-16-31(21-37,29(40)36(5)35(3)4)19-22-12-7-6-8-13-22/h6-10,12-15,20,26,33H,11,16-19,21,32H2,1-5H3,(H,34,39)/t26-,31-/m1/s1. InChi Key: VQPFSIRUEPQQPP-MXBOTTGLSA-N.