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AdipoRon

现货
Catalog No.
B1879
AdipoR1/2激动剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 500.00
现货
10mg
¥ 550.00
现货
50mg
¥ 2,380.00
现货

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Background

AdipoRon is an agonist of AdipoR1 and AdipoR2 with Kd values of 1.8 and 3.1 μM, respectively [1].

Adiponectin receptor (AdipoR) is a receptor for adiponectin, which is a protein and plays an important role in regulating glucose levels and fatty acid breakdown.

AdipoRon is the first orally active AdipoR1 and AdipoR2 agonist. AdipoRon (5-50 μM) increased AMPK phosphorylation via AdipoR1 in a dose-dependent way. Also, AdipoRon replenished adiponectin-stimulated AMPK phosphorylation. In C2C12 myotubes, AdipoRon increased PGC-1α expression and mitochondrial DNA content in a Ca2+- and dose-dependent way [1].

In wild-type mice, AdipoRon (50mg/kg) significantly induced AMPK phosphorylation in liver and skeletal muscle. Also, AdipoRon (50mg/kg) significantly reduced fasting plasma insulin and glucose levels. In wild-type mice fed a high-fat diet, AdipoRon increased the expression levels of

PPAR-α via AdipoR2 and reduced plasma levels of free fatty acid (FFA) and triglycerides. Also, AdipoRon reduced the expression levels of pro-inflammatory cytokines such as TNF-α and MCP-1 in the liver. In db/db obese mice, AdipoRon significantly reduced plasma glucose levels and ameliorated insulin resistance, glucose intolerance and dyslipidaemia [1]. In wild type mice, AdipoRon significantly improved cardiac function and inhibited myocardial ischemia/reperfusion (MI/R)-induced apoptosis [2].

References:
[1].  Okada-Iwabu M, Yamauchi T, Iwabu M, et al. A small-molecule AdipoR agonist for type 2 diabetes and short life in obesity. Nature, 2013, 503(7477): 493-499.
[2].  Zhang Y, Zhao J, Li R, et al. AdipoRon, the First Orally Active Adiponectin Receptor Activator, Attenuates Post-Ischemic Myocardial Apoptosis. Am J Physiol Endocrinol Metab, 2015, ajpendo.00577.2014.

Chemical Properties

StorageStore at -20°C
M.Wt428.52
Cas No.924416-43-3
FormulaC27H28N2O3
Solubility≥21.45mg/mL in DMSO
Chemical Name2-(4-benzoylphenoxy)-N-(1-benzylpiperidin-4-yl)acetamide
SDFDownload SDF
Canonical SMILESO=C(C1=CC=C(OCC(NC2CCN(CC3=CC=CC=C3)CC2)=O)C=C1)C4=CC=CC=C4
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

L02肝细胞,RAW264.7巨噬细胞

溶解方法

该化合物在DMSO中的溶解度大于21.5 mg/mL。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。

反应条件

5–50 μM

应用

AdipoRon(5-50 μM)预处理以剂量依赖性方式减弱L02细胞系中TNF-α和TGF-β1的表达。在巨噬细胞中,AdipoRon以剂量依赖性方式显著抑制细胞生长。

动物实验 [2]:

动物模型

成年雄性WT小鼠和APN敲除(APN-/-)小鼠

给药剂量

口服,40 mg/kg

应用

口服给药AdipoRon显著改善野生型(WT)以及脂联素敲除(APN-/-)和心肌细胞特异性AMPKα2突变体转基因小鼠(AMPK-DN)的心脏功能恢复。口服AdipoRon显著减轻缺血后心脏细胞凋亡。在APN缺陷小鼠中,AdipoRon营救增强的心肌细胞凋亡。AdipoRon显著降低NADPH氧化酶表达,并抑制缺血/再灌注心脏中的超氧化物生成。

注意事项

由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。

References:

[1]. Wang Y, Wan Y, Ye G, et al. Hepatoprotective effects of AdipoRon against d-galactosamine-induced liver injury in mice[J]. European Journal of Pharmaceutical Sciences, 2016, 93: 123-131.

[2]. Zhang Y, Zhao J, Li R, et al. AdipoRon, the first orally active adiponectin receptor activator, attenuates postischemic myocardial apoptosis through both AMPK-mediated and AMPK-independent signalings[J]. American Journal of Physiology-Endocrinology and Metabolism, 2015, 309(3): E275-E282.

质量控制

化学结构

AdipoRon