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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
AdipoRon (also known as SC-396658) is a novel, first-in-class, and orally bioavailable adiponectin receptor agonist with KD of 1.8 and 3.1 μM for AdipoR1 and AdipoR2, respectively. 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.
| ln Vitro |
With Kds of 1.8 and 3.1 μM, AdipoRon is an oral AdipoR agonist that is both selective and active against AdipoR1 and AdipoR2. Through AdipoR1, AdipoRon (50 nM–50 μM) raises AMPK phosphorylation[1]. In L02 cells, AdipoRon (50 μM) attenuates TNF-α and TGF-β1 production in a dose-dependent manner. On macrophages, AdipoRon shows a notable and dosage-dependent proliferation suppression[2]. Treatment with AdipoRon dramatically reduces post-MI apoptosis and enhances cardiac functional recovery following reperfusion[3]. AdipoRon causes vasorelaxation and vasodilation through different pathways than adiponectin, all without significantly lowering VSMC [Ca2+]i[4].
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| ln Vivo |
In wild-type mice's skeletal muscle and liver, AdipoRon (50 mg/kg, iv) significantly phosphorylates AMPK, but not in Adipor1−/− or Adipor2−/− double-knockout mice[1]. AdipoRon (0.02, 0.1, and 0.5 mg/kg, ig) protects the hepatic architecture from distortion in response to D-GalN exposure and reduces the hepatotoxicity caused by D-GalN in mice. AdipoRon's hepatoprotective activity is most noticeable at higher dosages (0.1 and 0.5 mg/kg)[2]. AdipoRon (50 mg/kg, po) treatment rescues APN-deficient mice from enhanced cardiomyocyte apoptosis. In AMPK-DN mice, AdipoRon's antiapoptotic impact is diminished but not eliminated[3].
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| References |
[1]. Okada-Iwabu M, et al. A small-molecule AdipoR agonist for type 2 diabetes and short life in obesity. Nature. 2013 Nov 28;503(7477):493-9.
[2]. Wang Y, et al. Hepatoprotective effects of AdipoRon against d-galactosamine-induced liver injury in mice. Eur J Pharm Sci. 2016 Aug 9;93:123-131. [3]. Zhang Y, et al. AdipoRon, the first orally active adiponectin receptor activator, attenuates postischemic myocardial apoptosis through both AMPK-mediated and AMPK-independent signalings. Am J Physiol Endocrinol Metab. 2015 Aug 1;309(3):E275-82. [4]. Hong K, et al. Adiponectin Receptor Agonist, AdipoRon, Causes Vasorelaxation Predominantly Via a Direct Smooth Muscle Action. Microcirculation. 2016 Apr;23(3):207-20 |
| Molecular Formula |
C27H28N2O3
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| Molecular Weight |
428.52
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| CAS # |
924416-43-3
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| Related CAS # |
AdipoRon hydrochloride;1781835-20-8
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| SMILES |
O=C(C([H])([H])OC1C([H])=C([H])C(C(C2C([H])=C([H])C([H])=C([H])C=2[H])=O)=C([H])C=1[H])N([H])C1([H])C([H])([H])C([H])([H])N(C([H])([H])C2C([H])=C([H])C([H])=C([H])C=2[H])C([H])([H])C1([H])[H]
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| InChi Key |
SHHUPGSHGSNPDB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C27H28N2O3/c30-26(28-24-15-17-29(18-16-24)19-21-7-3-1-4-8-21)20-32-25-13-11-23(12-14-25)27(31)22-9-5-2-6-10-22/h1-14,24H,15-20H2,(H,28,30)
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| Chemical Name |
2-(4-benzoylphenoxy)-N-(1-benzylpiperidin-4-yl)acetamide
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.83 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.85 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.85 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.08 mg/mL (4.85 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL corn oil and mix evenly. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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