MaciMorelin Acetate

Product NameMaciMorelin Acetate
CAS945212-59-9
MFC28H34N6O5
MW534.60676
EINECS
MOL File945212-59-9.mol

Chemical Properties

storage temp.	-10 to -25°C
solubility	DMSO: 2mg/mL, clear
form	Solid
color	White to off-white
InChIKey	UJVDJAPJQWZRFR-DHIUTWEWSA-N
SMILES	[nH]1c2c(c(c1)C[C@@H](NC(=O)[C@H](NC(=O)C(N)(C)C)Cc3c4c([nH]c3)cccc4)NC=O)cccc2

Safety Information

WGK Germany	WGK 3
Storage Class	11 - Combustible Solids

Usage And Synthesis

Uses

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

Biological Activity

Macimorelin (AEZS-130; ARD-07; EP1572; UMV1843; Aib-DTrp-DgTrp-CHO) is an orally active peptido-mimetic growth hormone (GH) secretagogue (GHS) th at targets human and animal GHS-receptor (IC50 in nM = 10.2/ghrelin, 12.3/hexaghrelin, 15.6/macimorelin against ghrelin binding to human GHS-R) with potent and selective GH-releasing activity in vivo (GH level = 158.8 μg/L 15 min post 300 μg/kg s.c. in neonatal rats; 11.3 μg/L without treatment).

in vivo

Macimorelin (5 mg/kg, i.p. twice daily for 2 weeks) acetate decreased 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. DOI:10.1210/jc.2018-00665
[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. DOI:10.1111/ene.14992
[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:

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