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  • Product Name: AdipoRon
  • Price: $300.0/100mg $600.0/250mg $1200.0/1g
  • Purity: 98.0%
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924416-43-3

924416-43-3 structure
924416-43-3 structure
  • Name: AdipoRon
  • Chemical Name: Acetamide, 2-​(4-​benzoylphenoxy)​-​N-​[1-​(phenylmethyl)​-​4-​piperidinyl]​-
  • CAS Number: 924416-43-3
  • Molecular Formula: C27H28N2O3
  • Molecular Weight: 428.523
  • Catalog: Signaling Pathways GPCR/G Protein Adiponectin Receptor
  • Create Date: 2017-09-07 10:04:30
  • Modify Date: 2024-01-03 06:24:29
  • AdipoRon is an orally active adiponectin receptor (AdipoR) agonist, binding to AdipoR1 and AdipoR2 with Kds of 1.8 and 3.1 μM, respectively.
Name Acetamide, 2-​(4-​benzoylphenoxy)​-​N-​[1-​(phenylmethyl)​-​4-​piperidinyl]​-
Synonyms 2-(4-Benzoylphenoxy)-N-(1-benzyl-4-piperidinyl)acetamide
Acetamide, 2-(4-benzoylphenoxy)-N-[1-(phenylmethyl)-4-piperidinyl]-
AdipoRon
SC-396658
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.
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℃
Symbol GHS07 GHS09
GHS07, GHS09
Signal Word Warning
Hazard Statements H302-H410
Precautionary Statements P273-P501
RIDADR UN 3077 9 / PGIII

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title: CAS No. 924416-43-3 | Chemsrc address: https://m.chemsrc.com/en/baike/1172698.html

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