AdipoRon |
Catalog No.GC10254
One-Click Copy Product Info
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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.
Products are for research use only. Not for human use. We do not sell to patients.
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.
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Cell experiment [1]: |
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Cell lines |
Saos-2 and U2OS cells |
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Preparation method |
Saos-2 and U2OS growth curves were determined after treatment with 20μg/mL AdipoRon for 24, 48 and 72 hours. |
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Reaction Conditions |
20μg/mL; 24, 48 and 72 h |
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Applications |
AdipoRon inhibit proliferation in Saos-2 and U2OS Osteosarcoma Cells. |
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Animal experiment [2]: |
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Animal models |
APN-KO、AMPK-DN mice |
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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). |
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Dosage form |
50mg/kg; p.o. |
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Applications |
Oral administration of AdipoRon to mice significantly improved cardiac function and attenuated postischemic cardiomyocyte apoptosis. |
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References: |
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| Cas No. | 924416-43-3 | SDF | |
| Chemical Name | 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 | ||
| Formula | C27H28N2O3 | M.Wt | 428.52 |
| Solubility | ≥ 100mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3336 mL | 11.6681 mL | 23.3361 mL |
| 5 mM | 466.7 μL | 2.3336 mL | 4.6672 mL |
| 10 mM | 233.4 μL | 1.1668 mL | 2.3336 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 15 reference(s) in Google Scholar.)