| Identification | Back Directory | [Name]
MaciMorelin Acetate | [CAS]
945212-59-9 | [Synonyms]
EP-1572 acetate
MaciMorelin Acetate
AEZS-130 acetate|||AEZS-130 acetate|||EP-1572 acetate | [Molecular Formula]
C28H34N6O5 | [MDL Number]
MFCD28502054 | [MOL File]
945212-59-9.mol | [Molecular Weight]
534.607 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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/ghrelin12.3/hexaghrelin15.6/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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| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
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