Leriglitazone-d4

Modify Date: 2024-01-08 11:32:33

Leriglitazone-d4 Structure
Leriglitazone-d4 structure
Common Name Leriglitazone-d4
CAS Number 1188263-49-1 Molecular Weight 376.46
Density N/A Boiling Point N/A
Molecular Formula C19H16D4N2O4S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Leriglitazone-d4


Leriglitazone-d4 is deuterium labeled Leriglitazone. Leriglitazone (Hydroxypioglitazone), a metabolite of pioglitazone.Leriglitazone (Hydroxypioglitazone) 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) binds to the PPARγ C-terminal ligand-binding domain (LBD) with Ki of 1.2 μM,induces transcriptional efficacy of the PPARγ (LBD) with EC50 of 680 nM[1].

 Names

Name 5-[[2,3,5,6-tetradeuterio-4-[2-[5-(1-hydroxyethyl)pyridin-2-yl]ethoxy]phenyl]methyl]-1,3-thiazolidine-2,4-dione
Synonym More Synonyms

 Leriglitazone-d4 Biological Activity

Description Leriglitazone-d4 is deuterium labeled Leriglitazone. Leriglitazone (Hydroxypioglitazone), a metabolite of pioglitazone.Leriglitazone (Hydroxypioglitazone) 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) binds to the PPARγ C-terminal ligand-binding domain (LBD) with Ki of 1.2 μM,induces transcriptional efficacy of the PPARγ (LBD) with EC50 of 680 nM[1].
Related Catalog
In Vitro Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
References

[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

[2]. 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 C19H16D4N2O4S
Molecular Weight 376.46
Exact Mass 376.13900
PSA 117.31000
LogP 2.92640

 Synonyms

Hydroxy Pioglitazone Labeled d4