AdipoRon
目录号 : GC10254
An adiponectin receptor agonist
Cas No.:924416-43-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
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Cell lines |
L02 hepatocytes, RAW264.7 macrophages |
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Preparation method |
The solubility of this compound in DMSO is >21.5mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
5–50 μM |
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Applications |
AdipoRon (5–50 μM) pretreatment dose-dependently attenuated the expression of TNF-α and TGF-β1 in L02 cell line. AdipoRon exhibited significant and dosage-dependent growth suppression on macrophages. |
| Animal experiment [2]: | |
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Animal models |
Adult male WT mice and APN knockout (APN-/-) mice |
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Dosage form |
Oral administration, 40 mg/kg |
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Application |
Oral administration of AdipoRon significantly improved cardiac functional recovery in wild-type (WT), adiponectin knockout (APN-/-), and cardiomyocyte-specific AMPKα2 mutant transgenic mice (AMPK-DN). Oral AdipoRon administration significantly attenuated postischemic cardiac apoptosis. AdipoRon rescued the enhanced cardiomyocyte apoptosis in APN-deficient mice. AdipoRon significantly reduced NADPH oxidase expression and inhibited superoxide production in ischemic/reperfused heart. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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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. |
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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.
| Cas No. | 924416-43-3 | SDF | |
| 化学名 | 2-(4-benzoylphenoxy)-N-(1-benzylpiperidin-4-yl)acetamide | ||
| Canonical SMILES | O=C(C1=CC=C(OCC(NC2CCN(CC3=CC=CC=C3)CC2)=O)C=C1)C4=CC=CC=C4 | ||
| 分子式 | C27H28N2O3 | 分子量 | 428.52 |
| 溶解度 | ≥ 21.45mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3336 mL | 11.6681 mL | 23.3361 mL |
| 5 mM | 0.4667 mL | 2.3336 mL | 4.6672 mL |
| 10 mM | 0.2334 mL | 1.1668 mL | 2.3336 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。