AdipoRon


CAS No. : 924416-43-3

AdipoRon,924416-43-3
Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I000029
Synonyms:2-(4-benzoylphenoxy)-N-(1-benzylpiperidin-4-yl)acetamide
Molecular Formula:C27H28N2O3
Molecular Weight:428.5
Target:Adiponectin Receptor
IC50:1.8/3.1 uM(AdipoR1/2, Kd)
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Appearance:Solid powder
Purity: > 98%
Cat No:I000029
Cas No:924416-43-3
Product-Name:AdipoRon
InChI: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)
InChIKey:SHHUPGSHGSNPDB-UHFFFAOYSA-N
SMILES:O=C(C1=CC=C(OCC(NC2CCN(CC3=CC=CC=C3)CC2)=O)C=C1)C4=CC=CC=C4

AdipoRon(cas 924416-43-3) is a novel small-molecule AdipoR agonist; binds to both AdipoR1(Kd= 1.8 uM) and AdipoR2(Kd=3.1 uM). 

in vitro: The treatment of C2C12myotubes withAdipoRon caused an increase in the phosphorylation of Thr 172 in the a-subunit of AMPK (aAMPK). AdipoRon at concentrations of 5–50 mM increased AMPK phosphorylation in a dose-dependent manner to almost the same extent as did adiponectin. Suppression of AdipoR1 by specific siRNA greatly reduced the increase in AMPK phosphorylation induced by AdipoRon. In the presence or absence of the submaximal concentration of adiponectin (15 ug/ml), AdipoRon increased AMPK phosphorylation in a dose-dependent manner, whereas AdipoRon did not increase nor decrease AMPK phosphorylation in the presence of the maximal concentration of adiponectin (50 ug/ml) [1]. 

in vivo: Oral administration of AdipoRon (50 mg /kg body weight) for 10 days did not significantly affect body weight nor food intake in mice on a high-fat diet, but it did significantly reduce fasting plasma glucose and insulin levels as well as glucose and insulin responses during oral glucose tolerance tests in wild-type mice treated with AdipoRon [1].


1:AdipoRon may be benefit for atherosclerosis prevention. Esfahani M, Shabab N, Saidijam M.Iran J Basic Med Sci. 2017 Feb;20(2):107-109. doi: 10.22038/ijbms.2017.8228. PMID: 28293385 Free PMC Article
2:AdipoRon, an adiponectin receptor agonist, attenuates PDGF-induced VSMC proliferation through inhibition of mTOR signaling independent of AMPK: Implications toward suppression of neointimal hyperplasia. Fairaq A, Shawky NM, Osman I, Pichavaram P, Segar L.Pharmacol Res. 2017 May;119:289-302. doi: 10.1016/j.phrs.2017.02.016. Epub 2017 Feb 22. PMID: 28237515
3:Promigratory and proangiogenic effects of AdipoRon on bone marrow-derived mesenchymal stem cells: an in vitro study. Malih S, Saidijam M, Mansouri K, Pourjafar M, Tafakh MS, Talebzadeh F, Najafi R.Biotechnol Lett. 2017 Jan;39(1):39-44. doi: 10.1007/s10529-016-2214-0. Epub 2016 Sep 15. PMID: 27627895
4:Hepatoprotective effects of AdipoRon against d-galactosamine-induced liver injury in mice. Wang Y, Wan Y, Ye G, Wang P, Xue X, Wu G, Ye B.Eur J Pharm Sci. 2016 Oct 10;93:123-31. doi: 10.1016/j.ejps.2016.08.017. Epub 2016 Aug 9. PMID: 27516150
5:Identification and characterization of in vitro and in vivo generated metabolites of the adiponectin receptor agonists AdipoRon and 112254. Dib J, Thomas A, Delahaut P, Fichant E, Schänzer W, Thevis M.J Pharm Biomed Anal. 2016 Jun 5;125:68-76. doi: 10.1016/j.jpba.2016.03.027. Epub 2016 Mar 14. PMID: 27003122
6:Adiponectin Receptor Agonist, AdipoRon, Causes Vasorelaxation Predominantly Via a Direct Smooth Muscle Action. Hong K, Lee S, Li R, Yang Y, Tanner MA, Wu J, Hill MA.Microcirculation. 2016 Apr;23(3):207-20. doi: 10.1111/micc.12266. PMID: 26728950
7:AdipoRon: a possible drug for colorectal cancer prevention? Malih S, Najafi R.Tumour Biol. 2015 Sep;36(9):6673-5. doi: 10.1007/s13277-015-3911-3. Epub 2015 Aug 18. PMID: 26282004
8:AdipoRon, the first orally active adiponectin receptor activator, attenuates postischemic myocardial apoptosis through both AMPK-mediated and AMPK-independent signalings. Zhang Y, Zhao J, Li R, Lau WB, Yuan YX, Liang B, Li R, Gao EH, Koch WJ, Ma XL, Wang YJ.Am J Physiol Endocrinol Metab. 2015 Aug 1;309(3):E275-82. doi: 10.1152/ajpendo.00577.2014. Epub 2015 Jun 2. PMID: 26037251 Free PMC Article
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