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Merck
CN

SML3680

Macimorelin acetate

≥98% (HPLC)

别名:

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 acetate, 2-Methylalanyl-N-[(1R)-1-(formylamino)-2-(1H-indol-3-yl)ethyl]-D-tryptophanamide acetate, AEZS 130 acetate, AEZS-130 acetate, AEZS130 acetate, ARD 07 acetate, ARD-07 acetate, ARD07 acetate, Aib-DTrp-DgTrp-CHO acetate, EP 1572 acetate, EP-1572 acetate, EP1572 acetate, JMV 1843 acetate, JMV-1843 acetate, JMV1843 acetate, UMV 1843 acetate, UMV-1843 acetate, UMV1843 acetate

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关于此项目

经验公式（希尔记法）:
C26H30N6O3 · xC2H4O2
分子量:
474.55 (free base basis)
UNSPSC Code:
51111800
NACRES:
NA.77
MDL number:
MFCD09260160

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产品名称

Macimorelin acetate, ≥98% (HPLC)

SMILES string

[nH]1c2c(c(c1)C[C@@H](NC(=O)[C@H](NC(=O)C(N)(C)C)Cc3c4c([nH]c3)cccc4)NC=O)cccc2

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

InChI key

UJVDJAPJQWZRFR-DHIUTWEWSA-N

assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

-10 to -25°C

Quality Level

100

相关类别

Biochem/physiol Actions

Macimorelin (AEZS-130; ARD-07; EP1572; UMV1843; Aib-DTrp-DgTrp-CHO) is an orally active peptido-mimetic growth hormone (GH) secretagogue (GHS) that 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).
Orally active peptido-mimetic growth hormone (GH) secretagogue (GHS) with potent and selective GH-releasing efficacy in vivo by targeting GHS-receptor.

Disclaimer

Hygroscopic

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

法规信息

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历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
0000311115
0000311115
0000244955
0000239726
0000244955

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Ghrelin stimulation of growth hormone-releasing hormone neurons is direct in the arcuate nucleus
PLoS ONE, 5(2), e9159-e9159 (2010)
F Broglio et al.
Journal of endocrinological investigation, 25(8), RC26-RC28 (2002-09-21)
EP1572 UMV1843 [Aib-DTrp-DgTrp-CHO]) is a new peptido-mimetic GH secretagogue (GHS) showing binding potency to the GHS-receptor in animal and human tissues similar to that of ghrelin and peptidyl GHS. EP1572 induces marked GH increase after s.c. administration in neonatal rats.
M Holubová et al.
Physiological research, 62(4), 435-444 (2013-04-18)
Ghrelin and agonists of its receptor GHS-R1a are potential substances for the treatment of cachexia. In the present study, we investigated the acute and long term effects of the GHS R1a agonist JMV 1843 (H Aib-DTrp-D-gTrp-CHO) on food intake, body
An Buckinx et al.
European journal of neurology, 28(9), 3100-3112 (2021-06-23)
Current drugs for epilepsy affect seizures, but no antiepileptogenic or disease-modifying drugs are available that prevent or slow down epileptogenesis, which is characterized by neuronal cell loss, inflammation and aberrant network formation. Ghrelin and ghrelin receptor (ghrelin-R) agonists were previously
Valeria Sibilia et al.
Amino acids, 43(4), 1751-1759 (2012-03-13)
Recent research suggests a role for ghrelin in the modulation of inflammatory disorders. However, the type of ghrelin receptor (GHS-R) involved in both the anti-inflammatory and anti-hyperalgesic actions of ghrelin remains to be characterized. In this study, we examined whether
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