MedChemExpress LLC (MCE)

MedChemExpress - Model Azemiglitazone - 1133819-87-0

Azemiglitazone (MSDC-0602) is an orally active thiazolidinedione (TZD) -like molecule, which binds to PPARγ with low binding and activating affinity. Azemiglitazone inhibits mitochondrial pyruvate carrier (MPC), which inhibits Alzheimer’s disease and diminishes nonalcoholic steatohepatitis (NASH) caused liver injury[4][5].

Azemiglitazone

MCE China：Azemiglitazone

Brand：MedChemExpress (MCE)

Cat. No.HY-108022

CAS：1133819-87-0

Synonyms：MSDC-0602

Purity：97.35%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Azemiglitazone (MSDC-0602) is an orally active thiazolidinedione (TZD) -like molecule, which binds to PPARγ with low binding and activating affinity. Azemiglitazone inhibits mitochondrial pyruvate carrier (MPC), which inhibits Alzheimer’s disease and diminishes nonalcoholic steatohepatitis (NASH) caused liver injury.

In Vitro：Azemiglitazone (15 μM, 4 h) crosslinks specifically to MPC, inhibits pyruvate oxidation and glucose production in liver mitochondria with interaction with MPC2[3]. Azemiglitazone has low binding and activating affinity for PPARγ with IC50 of 18.25 μM[6].

In Vivo：Azemiglitazone (2-5 μM in blood, p.o for 2-4 weeks) improves insulin sensitivity in striated muscle, adipose tissue, and liver of DIO C57BL/6 mice[6]. Azemiglitazone (2-5 μM in blood, p.o for 2-4 weeks) improves mitochondrial respiratory rate in DIO C57BL/6 mice[6]. Azemiglitazone reduces NASH caused liver injury, prevents (2-5 μM in blood, p.o. for 12 weeks) and reverses (2-5 μM in blood, p.o. for 3 weeks) stellate cells activation and fibrosis in HTF-C diet feeding C57BL6/J mice[4]. Azemiglitazone (2-5 μM in blood, p.o.) causes weight loss and suppresses stellate cell activation with or without MPC function in HTF-C diet feeding LS-Mpc2-/-C57BL6/J mice[4].

References：

[1]. Chen Z, et al. Resistance and metabolic derangements in obese mice are ameliorated by a novel peroxisome proliferator-activated receptor γ-sparing thiazolidinedione. J Biol Chem. 2012 Jul 6;287(28):23537-48. [Content Brief]

[2]. Vigueira PA, et al. The beneficial metabolic effects of sensitizers are not attenuated by mitochondrial pyruvate carrier 2 hypomorphism. Exp Physiol. 2017 Aug 1;102(8):985-999. [Content Brief]

[3]. McCommis KS, et al., Loss of Mitochondrial Pyruvate Carrier 2 in the Liver Leads to Defects in Gluconeogenesis and Compensation via Pyruvate-Alanine Cycling. Cell Metab. 2015 Oct 6;22(4):682-94. [Content Brief]

[4]. McCommis KS, et al., Targeting the mitochondrial pyruvate carrier attenuates fibrosis in a mouse model of nonalcoholic steatohepatitis. Hepatology. 2017 May;65(5):1543-1556. [Content Brief]

[5]. Phelix, C., et al., MSDC-0160 and MSDC-0602 binding with human mitochondrial pyruvate carrier (MPC) 1 and 2 heterodimer: PPARγ activating and sparing TZDs as therapeutics. Int. J. Knowl. Knowl. Bioinform.2017, 7, 43–67.

[6]. Chen Z, et al., Insulin resistance and metabolic derangements in obese mice are ameliorated by a novel peroxisome proliferator-activated receptor γ-sparing thiazolidinedione. J Biol Chem. 2012 Jul 6;287(28):23537-48. [Content Brief]

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