AdipoRon

Modify Date: 2024-01-03 06:24:29

AdipoRon Structure
AdipoRon structure
Common Name AdipoRon
CAS Number 924416-43-3 Molecular Weight 428.523
Density 1.2±0.1 g/cm3 Boiling Point 645.3±55.0 °C at 760 mmHg
Molecular Formula C27H28N2O3 Melting Point N/A
MSDS USA Flash Point 344.1±31.5 °C
Symbol GHS07 GHS09
GHS07, GHS09
Signal Word Warning

 Use of AdipoRon


AdipoRon is an orally active adiponectin receptor (AdipoR) agonist, binding to AdipoR1 and AdipoR2 with Kds of 1.8 and 3.1 μM, respectively.

 Names

Name Acetamide, 2-​(4-​benzoylphenoxy)​-​N-​[1-​(phenylmethyl)​-​4-​piperidinyl]​-
Synonym More Synonyms

 AdipoRon Biological Activity

Description AdipoRon is an orally active adiponectin receptor (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 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

Density 1.2±0.1 g/cm3
Boiling Point 645.3±55.0 °C at 760 mmHg
Molecular Formula C27H28N2O3
Molecular Weight 428.523
Flash Point 344.1±31.5 °C
Exact Mass 428.209991
PSA 58.64000
LogP 4.14
Vapour Pressure 0.0±1.9 mmHg at 25°C
Index of Refraction 1.632
Storage condition -20℃

 Safety Information

Symbol GHS07 GHS09
GHS07, GHS09
Signal Word Warning
Hazard Statements H302-H410
Precautionary Statements P273-P501
RIDADR UN 3077 9 / PGIII

 Synonyms

2-(4-Benzoylphenoxy)-N-(1-benzyl-4-piperidinyl)acetamide
Acetamide, 2-(4-benzoylphenoxy)-N-[1-(phenylmethyl)-4-piperidinyl]-
AdipoRon
SC-396658
Top Suppliers:I want be here

  • DC Chemicals Limited
  • China
  • Product Name: AdipoRon
  • Price: $300.0/100mg $600.0/250mg $1200.0/1g
  • Purity: 98.0%
  • Stocking Period: 3 Day
  • Contact: Tony Cao


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Price: $79/10mM*1mLinDMSO

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