AdipoRon hydrochloride

Modify Date: 2024-04-01 23:43:25

AdipoRon hydrochloride Structure
AdipoRon hydrochloride structure
Common Name AdipoRon hydrochloride
CAS Number 1781835-20-8 Molecular Weight 464.984
Density N/A Boiling Point N/A
Molecular Formula C27H29ClN2O3 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of AdipoRon hydrochloride


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

 Names

Name AdipoRon hydrochloride
Synonym More Synonyms

 AdipoRon hydrochloride Biological Activity

Description AdipoRon hydrochloride is an orally active and specific AdipoR agonist, binding to AdipoR1 and AdipoR2, with Kds of 1.8 and 3.1 μM, respectively.
Related Catalog
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 Kds 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].
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].
Cell Assay 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].
Animal Admin 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].
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.

 Chemical & Physical Properties

Molecular Formula C27H29ClN2O3
Molecular Weight 464.984
Exact Mass 464.186676

 Synonyms

Acetamide, 2-(4-benzoylphenoxy)-N-[1-(phenylmethyl)-4-piperidinyl]-, hydrochloride (1:1)
2-(4-Benzoylphenoxy)-N-(1-benzyl-4-piperidinyl)acetamide hydrochloride (1:1)
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