Home Metabolism Mitochondrial pyruvate carrier inhibitor Azemiglitazone (MSDC-0602) For research use only.

Azemiglitazone (MSDC-0602)

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

Azemiglitazone (MSDC-0602) Chemical Structure

CAS: 1133819-87-0

Purity & Quality Control

Batch: S745401 DMSO] 82 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.52%
99.52

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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
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>
Kinase Assay 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 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.
In Vivo
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>

Chemical lnformation & Solubility

Molecular Weight 371.41 Formula

C19H17NO5S
CAS No. 1133819-87-0 SDF --
Smiles COC1=CC=CC(=C1)C(=O)COC2=CC=C(CC3SC(=O)NC3=O)C=C2
Storage (From the date of receipt) 3 years-21°C powder

In vitro
Batch:

DMSO : 82 mg/mL ( (220.78 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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