AdipoRon hydrochloride

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AdipoRon hydrochloride is an orally active and specific AdipoR agonist, binding to AdipoR1 and AdipoR2, with K_ds of 1.8 and 3.1 μM, respectively.

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AdipoRon hydrochloride Chemical Structure

CAS No. : 1781835-20-8

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Other In-stock Forms of AdipoRon hydrochloride:

AdipoRon

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AdipoRon In-stock

24 Publications Citing Use of MCE AdipoRon hydrochloride

: AdipoRon hydrochloride purchased from MedChemExpress. Usage Cited in: J Neurotrauma. 2019 Mar 19;36(6):903-918. [Abstract]; WT macrophages are incubated with myelin debris for 3 hours to obtain mye-MΦ, and further treated with AdipoRon for another 48 hours. ABCA1 and ABCG1 levels are assessed by western blot.

: AdipoRon hydrochloride purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2018 Apr 20;293(16):6064-6074. [Abstract]; Interaction of APPL1sv with adiponectin receptors in cells. Mouse hepatocytes are serum-starved for 4 h and treated with or without 50 μM AdipoRon (Ad) for 0, 5, or 10 min.

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Description	AdipoRon hydrochloride is an orally active and specific AdipoR agonist, binding to AdipoR1 and AdipoR2, with K_ds of 1.8 and 3.1 μM, respectively.
IC₅₀ & Target	Kd: 1.8 μM (AdipoR1), 3.1 μM (AdipoR2)^[1]
In Vitro	AdipoRon hydrochloride is an orally active and specific AdipoR agonist, binds to AdipoR1 and AdipoR2, with K_ds of 1.8 and 3.1 μM. AdipoRon (50 nM-50 μM) increases AMPK phosphorylation via AdipoR1^[1]. AdipoRon (50 μM) dose-dependently attenuates the expression of TNF-α and TGF-β1 in the L02 cells. AdipoRon exhibits significant and dosage-dependent growth suppression on macrophages^[2]. AdipoRon treatment significantly improves cardiac functional recovery after reperfusion, and inhibits post-MI apoptosis^[3]. AdipoRon exerts vasodilation by mechanisms distinct to adiponectin and induces vasorelaxation without a marked decrease in VSMC [Ca²⁺]_i^[4]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. AdipoRon hydrochloride Related Antibodies
In Vivo	AdipoRon (50 mg/kg, i.v.) cuases significant phosphorylation of AMPK in skeletal muscle and liver of wild-type mice but not Adipor1^−/− Adipor2^−/− double-knockout 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-GalN challenge. The hepatoprotective potential of AdipoRon is particularly evident in higher dosages (0.1 and 0.5 mg/kg)^[2]. Enhanced cardiomyocyte 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]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight	464.98
Formula	C₂₇H₂₉ClN₂O₃
CAS No.	1781835-20-8
SMILES	O=C(C1=CC=CC=C1)C2=CC=C(OCC(NC3CCN(CC4=CC=CC=C4)CC3)=O)C=C2.Cl
Shipping	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation	Data Sheet (274 KB) Handling Instructions (2659 KB)
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. [Content Brief] [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. [Content Brief] [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. [Content Brief] [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. [Content Brief]

Cell Assay ^[2]	The effects of AdipoRon on the proliferation of parenchymal and non-parenchymal hepatocytes are evaluated in vitro via L02 and RAW264.7, by MTT assay as described with slight modification: 100 μL cells suspension (6×10⁴/mL) are seeded in a 96-well plate and incubated for 18 h. Fresh media with AdipoRon are added at specified concentrations, and the incubations continue for a further 24 h. Then cells are incubated for 4 h with 0.5 mg/mL of MTT, and analyzed in a microplate reader at 490 nm. Each group is performed in six replications. The mean absorbance values corrected for a blank (medium only) are calculated as percentages of survival^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	Mice^[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 are dissolved in DMSO and diluted by saline containing 0.5% sodium carboxymethyl cellulose (CMC-Na) [final vehicle: 5% DMSO (v/v) saline solution]. All test groups are administered with vehicle (control and model groups) or therapeutic agents (bicyclol or AdipoRon groups) at a dosing volume of 10 mL/kg, by intragastric (i.g.) gavage twice per 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 of 600 mg/kg to induce acute liver injury, while the control group mice receive saline instead. Then mice are fasted for 20 h before orbital blood collection. Finally, all animals are sacrificed by cervical dislocation, and livers are harvested for biochemical or histopathology analysis^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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. [Content Brief] [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. [Content Brief] [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. [Content Brief] [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. [Content Brief]