Macimorelin

• CAT Number: I007900
• CAS Number: 381231-18-1
• Molecular Formula: C26H30N6O3
• Molecular Weight: 474.5548
• Purity: ≥95%
• Solubility: Soluble in DMSO, not in water
• Storage: 0 - 4 °C for short term, or -20 °C for long term
• IUPAC Name: 2-amino-N-[(2R)-1-[[(1R)-1-formamido-2-(1H-indol-3-yl)ethyl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-2-methylpropanamide
• InChI: InChI=1S/C26H30N6O3/c1-26(2,27)25(35)31-22(11-16-13-28-20-9-5-3-7-18(16)20)24(34)32-23(30-15-33)12-17-14-29-21-10-6-4-8-19(17)21/h3-10,13-15,22-23,28-29H,11-12,27H2,1-2H3,(H,30,33)(H,31,35)(H,32,34)/t22-,23-/m1/s1
• InChIKey: UJVDJAPJQWZRFR-DHIUTWEWSA-N
• SMILES: CC(C)(C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)NC(CC3=CNC4=CC=CC=C43)NC=O)N

Macimorelin (CAT: I007900), also known as AEZS-130, EP-1572, or JMV1843, is a novel synthetic small molecule, acting as a ghrelin agonist, that is orally active and stimulates the secretion of growth hormone (GH). Based on the results of Phase 1 studies, AEZS-130 has potential applications for treating cachexia, a condition frequently associated with severe chronic diseases such as cancer, chronic obstructive pulmonary disease, and AIDS. In addition to the therapeutic application, a Phase 3 trial with AEZS-130 as a diagnostic test for adult growth hormone deficiencies has been completed.

Overview of Clinical Research

Macimorelin is a Ghrelin receptor agonist. Macimorelin was licensed to Consilient Health in Europe and the United Kingdom in Dec 2020. 

Reference

1:The macimorelin-stimulated growth hormone test for adult growth hormone deficiency diagnosis. Agrawal V, Garcia JM.Expert Rev Mol Diagn. 2014 Jul;14(6):647-54. doi: 10.1586/14737159.2014.915746. Epub 2014 May 16. Review. PMID: 24834478
2:Macimorelin (AEZS-130)-stimulated growth hormone (GH) test: validation of a novel oral stimulation test for the diagnosis of adult GH deficiency. Garcia JM, Swerdloff R, Wang C, Kyle M, Kipnes M, Biller BM, Cook D, Yuen KC, Bonert V, Dobs A, Molitch ME, Merriam GR.J Clin Endocrinol Metab. 2013 Jun;98(6):2422-9. doi: 10.1210/jc.2013-1157. Epub 2013 Apr 4. PMID: 23559086 Free PMC Article