[CAS NO. 924416-43-3]  AdipoRon

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PRODUCTS SPECIFICATIONS [924416-43-3]

Catalog
HY-15848
Brand
MCE
CAS
924416-43-3

DESCRIPTION [924416-43-3]

Overview

MDLMFCD08271060
Molecular Weight428.52
Molecular FormulaC27H28N2O3
SMILESO=C(NC1CCN(CC2=CC=CC=C2)CC1)COC3=CC=C(C(C4=CC=CC=C4)=O)C=C3

For research use only. We do not sell to patients.


Summary

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


IC50 & 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 K d s 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 [Ca 2+ ] i [4] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.


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] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.


Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month

Solvent & Solubility

In Vitro:

DMSO : ≥ 44 mg/mL ( 102.68 mM )

H 2 O : < 0.1 mg/mL (insoluble)

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3336 mL 11.6681 mL 23.3361 mL
5 mM 0.4667 mL 2.3336 mL 4.6672 mL
10 mM 0.2334 mL 1.1668 mL 2.3336 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: 5% DMSO >> 40% PEG300 >> 5% Tween-80 >> 50% saline

    Solubility: ≥ 2.5 mg/mL (5.83 mM); Clear solution

  • 2.

    Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

    Solubility: ≥ 2.08 mg/mL (4.85 mM); Clear solution

  • 3.

    Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.85 mM); Clear solution

  • 4.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.85 mM); Clear solution

* All of the co-solvents are available by MCE.