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Macimorelin Acetate

Names

[ CAS No. ]:
381231-18-1

[ Name ]:
Macimorelin Acetate

[Synonym ]:
2-Methylalanyl-N-[(1R)-1-formamido-2-(1H-indol-3-yl)ethyl]-D-tryptophanamide
JMV 1843
Macimorelin
UNII-8680B21W73
D-Tryptophanamide, 2-methylalanyl-N-[(1R)-1-(formylamino)-2-(1H-indol-3-yl)ethyl]-
AEZS-130
Macimorelin Acetate

Biological Activity

[Description]:

Macimorelin (EP-1572), a GH secretagogue, is an orally active GHSR agonist. Macimorelin stimulates GH release. Macimorelin can be used in the research of adult growth hormone deficiency (AGHD), and Cancer anorexia-cachexia syndrome (CACS)[1][2][3].

[Related Catalog]:

Research Areas >> Cancer
Research Areas >> Endocrinology
Signaling Pathways >> GPCR/G Protein >> GHSR

[Target]

GHSR[1]


[In Vivo]

Macimorelin (5 mg/kg, i.p. twice daily for 2 weeks) decreases the number and duration of seizures in IHKA mouse model[2]. Animal Model: Intrahippocampal kainic acid (IHKA) mouse model[2] Dosage: 5 mg/kg Administration: Intraperitoneal injection (i.p.), twice daily for 2 weeks. Result: Significantly decreased the number and duration of seizures during the treatment period, but had no antiepileptogenic or disease-modifying effect.

[References]

[1]. Jose M Garcia, et al. Macimorelin as a Diagnostic Test for Adult GH Deficiency. J Clin Endocrinol Metab. 2018 Aug 1;103(8):3083-3093.

[2]. An Buckinx, et al. Translational potential of the ghrelin receptor agonist macimorelin for seizure suppression in pharmacoresistant epilepsy. Eur J Neurol. 2021 Sep;28(9):3100-3112.

[3]. Ali SA, Garcia JM. Randomized clinical trial of the novel oral ghrelin mimetic macimorelin in the treatment of cancer cachexia: study design and preliminary results. Endocr Rev. 2013;34:

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
948.6±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C26H30N6O3

[ Molecular Weight ]:
474.555

[ Flash Point ]:
527.5±34.3 °C

[ Exact Mass ]:
474.237946

[ PSA ]:
151.88000

[ LogP ]:
2.64

[ Vapour Pressure ]:
0.0±0.3 mmHg at 25°C

[ Index of Refraction ]:
1.676

Related Compounds