AdipoRon _Adiponectin Receptor Agonist - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAdipoRonCat. No.: HY-15848CAS No.: 924416-43-3分式: CHNO分量: 428.52作靶點(diǎn): Adiponectin Receptor作通路: GPCR/G Protein儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 44 mg/mL (102.68 mM)* means solub

2、le, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.3336 mL 11.6681 mL 23.3361 mL5 mM 0.4667 mL 2.3336 mL 4.6672 mL10 mM 0.2334 mL 1.1668 mL 2.3336 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 AdipoRon可服的脂聯(lián)素受體 (AdipoR) 激動劑，能夠與 AdipoR1 和 AdipoR2 結(jié)合，

3、Kd 值分別為 1.8 M和 3.1 M。IC50 & Target Kd: 1.8 M (AdipoR1), 3.1 M (AdipoR2) 1體外研究AdipoRon is an orally active and specific AdipoR agonist, binds to AdipoR1 and AdipoR2, with Kds of 1.8 and1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE3.1 M. AdipoRon (50 nM-50 M) increases AMPK phosphorylation via Adi

4、poR1 1. AdipoRon (50 M)dose-dependently attenuates the expression of TNF- and TGF-1 in the L02 cells. AdipoRon exhibitssignificant and dosage-dependent growth suppression on macrophages 2. AdipoRon treatment significantlyimproves cardiac functional recovery after reperfusion, and inhibits post-MI ap

5、optosis 3. AdipoRon exertsvasodilation by mechanisms distinct to adiponectin and induces vasorelaxation without a marked decrease inVSMC Ca2+i 4.體內(nèi)研究 AdipoRon (50mg/kg, i.v.) cuases significant phosphorylation of AMPK in skeletal muscle and liver of wild-type mice but not Adipor1/Adipor2/ double-kno

6、ckout mice 1. AdipoRon (0.02, 0.1, and 0.5 mg/kg, i.g.)alleviates D-GalN induced hepatotoxicity in mice, and prevents hepatic architecture distortion against D-GalNchallenge. The hepatoprotective potential of AdipoRon is particularly evident in higher dosages (0.1 and 0.5mg/kg) 2. Enhanced cardiomyo

7、cyte apoptosis in APN-deficient mice is rescued by AdipoRon (50 mg/kg,p.o.) administration. Antiapoptotic effect of AdipoRon is attenuated but not lost in AMPK-DN mice 3.PROTOCOLCell Assay 2 The effects of AdipoRon on the proliferation of parenchymal and non-parenchymal hepatocytes areevaluated in v

8、itro via L02 and RAW264.7, by MTT assay as described with slight modification: 100 L cellssuspension (6104/mL) are seeded in a 96-well plate and incubated for 18 h. Fresh media with AdipoRon areadded at specified concentrations, and the incubations continue for a further 24 h. Then cells are incubat

9、edfor 4 h with 0.5 mg/mL of MTT, and analyzed in a microplate reader at 490 nm. Each group is performed insix replications. The mean absorbance values corrected for a blank (medium only) are calculated aspercentages of survival 2.MCE has not independently confirmed the accuracy of these methods. The

10、y are for reference only.Animal Mice 2Administration 2 After 3 days of acclimation, mice are randomLy divided into six groups (9 mice in each): control, model,bicyclol (20 mg/kg), AdipoRon (0.02 mg/kg, 0.1 mg/kg, 0.5 mg/kg). The synthetic AdipoRon and bicyclol aredissolved in DMSO and diluted by sal

11、ine containing 0.5% sodium carboxymethyl cellulose (CMC-Na) finalvehicle: 5% DMSO (v/v) saline solution. All test groups are administered with vehicle (control and modelgroups) or therapeutic agents (bicyclol or AdipoRon groups) at a dosing volume of 10 mL/kg, by intragastric(i.g.) gavage twice per

12、day for three consecutive days prior to D-GalN administration. 2 h after last treatment,mice are challenged with a single intraperitoneal (i.p.) administration of D-GalN saline solution at a dose of600 mg/kg to induce acute liver injury, while the control group mice receive saline instead. Then mice

13、 arefasted for 20 h before orbital blood collection. Finally, all animals are sacrificed by cervical dislocation, andlivers are harvested for biochemical or histopathology analysis 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) J Biol Che

14、m. 2018 Apr 20;293(16):6064-6074. J Neurotrauma. 2019 Mar 19;36(6):903-918.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE Neurochem Res. 2019 May;44(5):1214-1227. Biomed Chromatogr. 2019 Jul 15:e4645.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Okada-Iwabu M, et al. A sma

15、ll-molecule AdipoR agonist for type 2 diabetes and short life in obesity. Nature. 2013 Nov28;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 Aug9;93:123-131.3. Zhang Y, et al. AdipoRon, the first orall

16、y active adiponectin receptor activator, attenuates postischemic myocardial apoptosis throughboth 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 Actio