Description

Leriglitazone-d4 (MIN-102-d4; Hydroxypioglitazone-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].–Applications-Metabolism-protein/nucleotide metabolism-Formula-C19H16D4N2O4S-Citation–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.-CASNumber-1188263-49-1-MolecularWeight-376.46-Compound Purity–SMILES-O=C(NC(S1)=O)C1CC2=C([2H])C([2H])=C(C([2H])=C2[2H])OCCC3=CC=C(C=N3)C(O)C-Research_Area-Metabolic Disease-Solubility-10 mM in DMSO-Target-Isotope-Labeled Compounds;PPAR-Isoform–Pathway-Cell Cycle/DNA Damage;Metabolic Enzyme/Protease;Others;Vitamin D Related/Nuclear Receptor-MCE Product type-Isotope-Labeled Compounds