AdipoRon
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
AdipoRon是AdipoR1和AdipoR2的激动剂,Kd值分别为1.8和3.1 μM[1].
脂联素受体(AdipoR)是脂联素的受体,是一种在调节葡萄糖水平和脂肪酸分解方面扮演重要角色的蛋白质.
AdipoRon是第一个口服有效的AdipoR1和AdipoR2激动剂.AdipoRon(5-50 μM)可通过AdipoR1以剂量依赖的方式增加AMPK的磷酸化.另外,AdipoRon可补充脂联素刺激的AMPK磷酸化.在C2C12肌小管中,AdipoRon可以Ca2+和剂量依赖的方式增加PGC-1α表达和线粒体DNA含量[1].
在野生型小鼠中,AdipoRon(50 mg/kg)可在肝脏和骨骼肌中显著诱导AMPK磷酸化.另外,AdipoRon(50 mg/kg)可显著降低空腹血浆胰岛素和葡萄糖水平.在饲喂高脂膳食的野生型小鼠中,AdipoRon可通过AdipoR2提高PPAR-α的表达水平,并能降低血浆游离脂肪酸(FFA)和甘油三酯水平.另外,AdipoRon可在肝脏中降低促炎细胞因子如TNF-α和MCP-1的表达水平.在db/db肥胖小鼠中,AdipoRon可显著降低血浆葡萄糖水平,并能改善胰岛素抵抗\葡萄糖耐受和血脂异常[1].在野生型小鼠中,AdipoRon可显著改善心脏功能,并抑制心肌缺血/再灌注(MI/R)导致的细胞凋亡[2].
参考文献:
[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.
Storage | Store at -20°C |
M.Wt | 428.52 |
Cas No. | 924416-43-3 |
Formula | C27H28N2O3 |
Solubility | ≥21.45 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O |
Chemical Name | 2-(4-benzoylphenoxy)-N-(1-benzylpiperidin-4-yl)acetamide |
SDF | Download SDF |
Canonical SMILES | O=C(C1=CC=C(OCC(NC2CCN(CC3=CC=CC=C3)CC2)=O)C=C1)C4=CC=CC=C4 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 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。溶液形式一般不宜长期储存,请尽快用完。 |
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. |
质量控制和MSDS
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