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Merck
CN
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安全信息

SML3680

Sigma-Aldrich

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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About This Item

经验公式（希尔记法）:
C26H30N6O3 · xC2H4O2
分子量:
474.55 (free base basis)
MDL编号:
MFCD09260160
UNSPSC代码:
51111800
UNSPSC代码:
12352200
NACRES:
NA.77

质量水平

100

方案

≥98% (HPLC)

表单

powder

储存条件

desiccated

颜色

white to beige

溶解性

DMSO: 2 mg/mL, clear

储存温度

-10 to -25°C

SMILES字符串

[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

生化/生理作用

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).

注意

Hygroscopic

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

法规信息

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分析证书(COA)

Lot/Batch Number
0000311115
0000311115
0000244955
0000239726
0000244955

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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.
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
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
Ghrelin stimulation of growth hormone-releasing hormone neurons is direct in the arcuate nucleus
PLoS ONE, 5(2), e9159-e9159 (2010)
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
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