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AdipoRon AdipoR agonist

Cat.No.S7365

AdipoRon (SC-396658) is a novel, and orally bioavailable adiponectin receptor agonist with KD of 1.8 and 3.1 μM for AdipoR1 and AdipoR2, respectively.
AdipoRon AdipoR agonist Chemical Structure

Chemical Structure

Molecular Weight: 428.52

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Quality Control

Batch: Purity: 99.96%
99.96

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (233.36 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 50 mg/mL

Water : Insoluble

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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Chemical Information, Storage & Stability

Molecular Weight 428.52 Formula

C27H28N2O3

Storage (From the date of receipt)
CAS No. 924416-43-3 Download SDF Storage of Stock Solutions

Synonyms SC-396658 Smiles C1CN(CCC1NC(=O)COC2=CC=C(C=C2)C(=O)C3=CC=CC=C3)CC4=CC=CC=C4

Mechanism of Action

Features
Orally bioavailable adiponectin receptor agonist that can be used for the treatment of obesity-related diseases.
Targets/IC50/Ki
AdipoR1
1.8 μM(Kd)
AdipoR2
3.1 μM(Kd)
In vitro
AdipoRon increases AMPK activation, PGC-1α expression and mitochondrial biogenesis by binding to both AdipoR1 and AdipoR2 in C2C12 myotubes.
In vivo
In skeletal muscle and liver of wild-type mice AdipoRon (50 mg/kg, i.v.) significantly induces phosphorylation of AMPK via AdipoR1 and AdipoR2. In WT mice, this compound (50 mg/kg, p.o.) improves insulin resistance, glucose intolerance and dyslipidaemia by activating AdipoR1–AMPK–PGC-1α pathways in skeletal muscle, while by activating AdipoR2–PPAR-α pathways in the liver. Moreover, this chemical ameliorates diabetes of genetically obese rodent model db/db mice, and prolongs the shortened lifespan of db/db mice on a high-fat diet.
References

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