| Identification | Back Directory | [Name]
MSDC-0602K | [CAS]
1314533-27-1 | [Synonyms]
MSDC-0602K
MSDC-0602 potassium
Azemiglitazone potassium
MSDC-0602K
(Azemiglitazone potassium) | [Molecular Formula]
C19H18KNO5S | [MOL File]
1314533-27-1.mol | [Molecular Weight]
411.51 |
| Hazard Information | Back Directory | [Uses]
Azemiglitazone potassium (MSDC-0602K), a PPARγ-sparing thiazolidinedione (Ps-TZD), binds to PPARγ with the IC50 of 18.25 μM[1]. Azemiglitazone potassium modulates the mitochondrial pyruvate carrier (MPC). Azemiglitazone potassium can be used for the research of fatty liver including dysfunctional lipid metabolism, inflammation, and insulin resistance[2]. Azemiglitazone potassium, an insulin sensitizer, improves insulinemia and fatty liver disease in mice, alone and in combination with Liraglutide[3]. | [in vivo]
Diabetic db/db and MS-NASH mice are treated with Azemiglitazone potassium by oral gavage, Liraglutide by s.c. injection, or combination Azemiglitazone potassium + Liraglutide. This combination treatment may be an effective therapeutic strategy for diabetes and non-alcoholic steatohepatitis (NASH). | Animal Model: | Five-week-old male db/db mice on C57BL/6J background and age/sex-matched db/+ control mice[1] | | Dosage: | 30 mg/kg MSDC-0602K; 0.2 mg/kg Liraglutide (obtained from MedChemExpress; HY-P0014) | | Administration: | MSDC-0602K gavage daily, Liraglutide s.c. injection every other day, or combined MSDC-0602K+ Liraglutide | | Result: | MSDC-0602K corrected glycemia and reduced insulinemia when given alone, or in combination with Liraglutide. However, MSDC-0602K + Liraglutide combination more significantly improved glucose tolerance and liver histology. |
| [IC 50]
PPAR-γ: 18.25 μM (IC50) | [References]
[1] Zhouji Chen, 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. DOI:10.1074/jbc.M112.363960
[2] Jerry R Colca, et al. MSDC-0602K, a metabolic modulator directed at the core pathology of non-alcoholic steatohepatitis. Expert Opin Investig Drugs. 2018 Jul;27(7):631-636. DOI:10.1080/13543784.2018.1494153
[3] Dakota R Kamm, et al. Novel insulin sensitizer MSDC-0602K improves insulinemia and fatty liver disease in mice, alone and in combination with liraglutide. J Biol Chem. Jan-Jun 2021;296:100807. DOI:10.1016/j.jbc.2021.100807 |
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