AdipoRon
目录号 : GC10254
AdipoRon是一种选择性、具有口服活性的脂联素受体（AdipoR）激动剂，对AdipoR1和AdipoR2的Kd值分别为1.8μM和3.1μM。
Cas No.:924416-43-3
Sample solution is provided at 25 µL, 10mM.
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AdipoRon is a selective, orally active adiponectin receptor (AdipoR) agonist with Kd values of 1.8μM and 3.1μM for AdipoR1 and AdipoR2, respectively[1]. AdipoRon has potential therapeutic effects in a variety of metabolic, cardiovascular and neurological diseases [2].
In vitro, AdipoRon (5-50μM) pretreated L02 cells attenuated the expression of TNF-α and TGF-β1 in a dose-dependent manner without cytotoxicity[3]. AdipoRon (20μg/mL) treated Saos-2 and U2OS osteosarcoma cells, significantly inhibited cell proliferation, and induced G0/G1 phase aggregation and S phase reduction[4]. AdipoRon (25μM) treated human luteinized granulosa cells, inhibited cell proliferation, increased phosphodiesterase activity, promoted cyclic adenosine monophosphate (cAMP) production and decreased estrogen secretion [5].
In vivo, AdipoRon (0.1 and 0.5 mg/kg) treatment in D-GalN-induced acute liver injury mice restored hepatic lesions, reduced pro-inflammatory macrophage infiltration, and decreased the expression of TNF-α, TGF-β1, IL-1β, and IL-6, while also promoting the activation of AMPK through phosphorylation[3]. AdipoRon (50 mg/kg) can significantly improve cardiac function and reduce post-ischemic cardiomyocyte apoptosis in mice treated with myocardial ischemia/reperfusion (MI/R) injury through oral administration [6].
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[J]. Nature, 2013, 503(7477): 493-499.
[2] Bhat I A, Kabeer S W, Reza M I, et al. AdipoRon: a novel insulin sensitizer in various complications and the underlying mechanisms: a review[J]. Current Molecular Pharmacology, 2020, 13(2): 94-107.
[3] Wang Y, Yu W, et al. Hepatoprotective effects of AdipoRon against d-galactosamine-induced liver injury in mice[J]. European Journal of Pharmaceutical Sciences, 2016.
[4] Sapio L, Nigro E, Ragone A, et al. AdipoRon affects cell cycle progression and inhibits proliferation in human osteosarcoma cells[J]. Journal of Oncology, 2020.
[5] Grandhaye J, Hmadeh S, Plotton I, et al. The adiponectin agonist, AdipoRon, inhibits steroidogenesis and cell proliferation in human luteinized granulosa cells[J]. Molecular and cellular endocrinology, 2021, 520: 111080.
[6] 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.
AdipoRon是一种选择性、具有口服活性的脂联素受体（AdipoR）激动剂，对AdipoR1和AdipoR2的Kd值分别为1.8μM和3.1μM[1]。AdipoRon在多种代谢、心血管和神经系统疾病中具有潜在治疗作用[2]。
在体外，AdipoRon（5-50μM）预处理L02细胞，以剂量依赖性方式减弱TNF-α和TGF-β1的表达，且无细胞毒性[3]。AdipoRon（20μg/mL）处理Saos-2和U2OS 骨肉瘤细胞，显著抑制了细胞增殖，并诱导G0/G1期聚集和S期减少[4]。AdipoRon（25μM）处理人类黄素化颗粒细胞，抑制了细胞增殖，提高了磷酸二酯酶活性，促进了环磷酸腺苷（cAMP）产生和雌激素分泌下降[5]。
在体内，AdipoRon（0.1和0.5mg/kg）治疗D-GalN诱导的急性肝损伤小鼠，恢复了肝病变，减少促炎巨噬细胞浸润，减少TNF-α、TGF-β1、白细IL-1β和IL-6的表达，同时通过磷酸化促进AMPK的激活[3]。AdipoRon（50mg/kg）通过口服治疗心肌缺血/再灌注（MI/R）损伤小鼠，显著改善心功能，减少缺血后心肌细胞凋亡[6]。
Cell experiment [1]: | |
Cell lines | Saos-2 and U2OS cells |
Preparation method | Saos-2 and U2OS growth curves were determined after treatment with 20μg/mL AdipoRon for 24, 48 and 72 hours. |
Reaction Conditions | 20μg/mL; 24, 48 and 72 h |
Applications | AdipoRon inhibit proliferation in Saos-2 and U2OS Osteosarcoma Cells. |
Animal experiment [2]: | |
Animal models | APN-KO、AMPK-DN mice |
Preparation method | Mice were anesthetized with 2% isoflurane. Myocardial ischemia/reperfusion (MI/R) was induced by temporarily exteriorizing the heart via a left thoracic incision, and placing a 6-0 silk suture slipknot around the left anterior descending coronary artery. Ten minutes before coronary occlusion, animals were randomized to receive either vehicle or AdipoRon (50mg/kg) via a gavage tube. After 30 min of MI, the slipknot was released. The myocardium was reperfused for either 3h (for all assays excluding cardiac functional measurement) or 24h (for cardiac functional assay). |
Dosage form | 50mg/kg; p.o. |
Applications | oral administration of AdipoRon to mice significantly improved cardiac function and attenuated postischemic cardiomyocyte apoptosis. |
References: [1] Sapio L, Nigro E, Ragone A, et al. AdipoRon affects cell cycle progression and inhibits proliferation in human osteosarcoma cells[J]. Journal of Oncology, 2020. [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. | |
| 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。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet