Azemiglitazone

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Chemical Structure| 1133819-87-0 同义名 : MSDC-0602
CAS号 : 1133819-87-0
货号 : A360389
分子式 : C19H17NO5S
纯度 : 98+%
分子量 : 371.41
MDL号 : MFCD28502493
存储条件：

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 120 mg/mL(323.1 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
描述 Azemiglitazone, also known as MSDC-0602, is an orally active thiazolidinedione (TZD)-like molecule with low binding and activation affinity for PPARγ. Azemiglitazone inhibits the mitochondrial pyruvate carrier (MPC), thereby inhibiting Alzheimer's disease and attenuating non-alcoholic steatohepatitis (NASH)-induced liver injury[4][5].At a concentration of 15 μM for 4 hours, Azemiglitazone cross-links specifically with MPC and inhibits pyruvate oxidation and glucose production in hepatic mitochondria by interacting with MPC2[3].Azemiglitazone has a low binding and activation affinity for PPARγ, with an IC50 of 18.25 μM[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.69mL

0.54mL

0.27mL

13.46mL

2.69mL

1.35mL

26.92mL

5.38mL

2.69mL
参考文献

[1]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.

[2]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.

[3]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.

[4]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.