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1-Hydroxy Pioglitazone Hydrochloride

Names

[ CAS No. ]:
146062-46-6

[ Name ]:
1-Hydroxy Pioglitazone Hydrochloride

[Synonym ]:
5-(4-{2-[5-(1-Hydroxyethyl)-2-pyridinyl]ethoxy}benzyl)-1,3-thiazolidine-2,4-dione hydrochloride (1:1)
2,4-Thiazolidinedione, 5-[[4-[2-[5-(1-hydroxyethyl)-2-pyridinyl]ethoxy]phenyl]methyl]-, hydrochloride (1:1)

Biological Activity

[Description]:

Leriglitazone (Hydroxypioglitazone) hydrochloride, a metabolite of pioglitazone. Leriglitazone (Hydroxypioglitazone) hydrochloride PioOH is a PPARγ agonist, stabilizes the PPARγ activation function-2 (AF-2) co-activator binding surface and enhances co-activator binding, affording slightly better transcriptional efficacy. Leriglitazone (Hydroxypioglitazone) hydrochloride binds to the PPARγ C-terminal ligand-binding domain (LBD) with a Ki of 1.2 μM，Leriglitazone induces transcriptional efficacy of the PPARγ (LBD) with an EC50 of 680 nM[1].

[Related Catalog]:

Signaling Pathways >> Cell Cycle/DNA Damage >> PPAR
Research Areas >> Metabolic Disease

[Target]

PPAR-γ


[References]

[1]. Mosure SA,et al. Structural Basis of Altered Potency and Efficacy Displayed by a Major in Vivo Metabolite of the Antidiabetic PPARγ Drug Pioglitazone. J Med Chem. 2019 Feb 28;62(4):2008-2023.

Chemical & Physical Properties

[ Molecular Formula ]:
C19H21ClN2O4S

[ Molecular Weight ]:
408.90

[ Exact Mass ]:
408.091064

Related Compounds