Home Metabolism Mitochondrial pyruvate carrier inhibitor Azemiglitazone (MSDC-0602)

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Azemiglitazone (MSDC-0602) Mitochondrial pyruvate carrier inhibitor

Cat.No.S7454

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

Azemiglitazone (MSDC-0602) Mitochondrial pyruvate carrier inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 371.41

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Quality Control

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

Solubility

In vitro
Batch:

DMSO : 82 mg/mL (220.78 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 371.41 Formula

C19H17NO5S

 Storage (From the date of receipt) 3 years-21°C powder
CAS No. 1133819-87-0 -- Storage of Stock Solutions

Synonyms N/A Smiles COC1=CC=CC(=C1)C(=O)COC2=CC=C(CC3SC(=O)NC3=O)C=C2

Mechanism of Action

Targets/IC50/Ki
MPC
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. This compound 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, this chemical only minimally activates Gal4-PPARγ in HepG2 cells even at a concentration of 50 μM.
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 this compound.
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 this compound also significantly improved glucose and insulin tolerance in ob/ob mice.
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