146062-46-6

146062-46-6 structure

Name: 1-Hydroxy Pioglitazone Hydrochloride
Chemical Name: 5-(4-{2-[5-(1-Hydroxyethyl)-2-pyridinyl]ethoxy}benzyl)-1,3-thiazolidine-2,4-dione hydrochloride (1:1)
CAS Number: 146062-46-6
Molecular Formula: C₁₉H₂₁ClN₂O₄S
Molecular Weight: 408.90
Catalog: Signaling Pathways Cell Cycle/DNA Damage PPAR
Create Date: 2018-06-19 11:50:59
Modify Date: 2024-01-02 11:20:23
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].

Name	5-(4-{2-[5-(1-Hydroxyethyl)-2-pyridinyl]ethoxy}benzyl)-1,3-thiazolidine-2,4-dione hydrochloride (1:1)
Synonyms	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)

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.