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Products Details
Product 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].
Web ID
– HY-117727S
Shipping
– Room temperature
Applications
– Metabolism-protein/nucleotide metabolism
Molecular Formula
– C19H16D4N2O4S
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.|[2]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.
CAS Number
– 1188263-49-1
Molecular Weight
– 376.46
SMILES
– O=C(NC(S1)=O)C1CC2=C([2H])C([2H])=C(C([2H])=C2[2H])OCCC3=CC=C(C=N3)C(O)C
Clinical Information
– No Development Reported
Research Area
– Metabolic Disease
Solubility
– 10 mM in DMSO
Target
– Isotope-Labeled Compounds;PPAR
Pathway
– Cell Cycle/DNA Damage;Others;Vitamin D Related/Nuclear Receptor
Product type
– Isotope-Labeled Compounds
Disclaimer: All products are for Research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation. Agdia Products are available for delivery only in Canada.
