Azemiglitazone (MSDC-0602)

Catalog No.S7454

For research use only.

Azemiglitazone (MSDC-0602) is a direct mitochondrial pyruvate carrier (MPC) inhibitor that modulates central carbon metabolism in mice and humans.

Azemiglitazone (MSDC-0602) Chemical Structure

CAS No. 1133819-87-0

Purity & Quality Control

Choose Selective Mitochondrial pyruvate carrier Inhibitors

Biological Activity

Description

Azemiglitazone (MSDC-0602) is a direct mitochondrial pyruvate carrier (MPC) inhibitor that modulates central carbon metabolism in mice and humans.

Targets
MPC [1]
In vitro

Azemiglitazone (MSDC-0602) is a modified hiazolidinediones (TZDP) with alterations in the carbon backbone that limit the ability to bind PPARγ, with the IC50 for PPARγ of 18.25 μM. Azemiglitazone (MSDC-0602) also shows the affinity for mitochondrial binding, with the IC50 of 1.38 μM. Using a Gal4-PPARγ construct containing the ligand binding domain of mouse PPARγ, MSDC-0602 only minimally activates Gal4-PPARγ in HepG2 cells even at a concentration of 50 μM.<sup><a class="sref" href="#s_ref">[1]</a></sup><sup><a class="sref" href="#s_ref">[2]</a></sup>

In vivo

Azemiglitazone (MSDC-0602) corrects plasma glucose, nonesterified fatty acids, triglycerides, cholesterol, and insulin concentrations, which are elevated in ob/ob mice compared with lean controls. Treatment with Azemiglitazone (MSDC-0602) also significantly improved glucose and insulin tolerance in ob/ob mice.<sup><a class="sref" href="#s_ref">[2]</a></sup>

Protocol (from reference)

Kinase Assay:

[2]

  • PPAR Binding Assays:

    TZD binding to the ligand binding domain of PPARγ was assessed in a LanthaScreen TMTR-FRET competitive binding assay performed according the protocol of the manufacturer (Invitrogen). IC 50 values for the PPARγ LanthaScreen were determined using Gen5 software (BioTek Instruments, Inc.). R2 values for individual IC50 values ranged from 0.983 to 0.999 based on three separate assays for each compound.

Cell Research:

[2]

  • Cell lines: HepG2 hepatoma cells
  • Concentrations: 0.5 nM, 5 nM, 50 nM, 0.5 μM, 5 μM and 50μM
  • Incubation Time: 48 h
  • Method:

    HepG2 hepatoma cells were co-transfected by calcium phosphate coprecipitation with expression vectors for Gal4-PPARγ (ligand binding domain only) or Gal4-PPARα, heterologous firefly luciferase reporter construct driven by five copies of a Gal4 response element, and  SV40-driven renilla luciferase reporter construct. Transfected cells were treated with PPARγ agonists (rosiglitazone and pioglitazone), PPARα agonist (GW7647), or MSDC-0602 for 24 h. Cell lysate firefly and renilla luciferase activity was assessed 48 h later by using the Dual-Glo kit. Firefly luciferase activity was corrected for renilla luciferase activity, and DMSO (vehicle) values were normalized to 1.0.

Chemical Information

Molecular Weight 371.41
Formula

C19H17NO5S

CAS No. 1133819-87-0
Storage 2 years -80 in solvent

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