Ertugliflozin-d9

Ertugliflozin-d9 is deuterated labeled Ertugliflozin (HY-15461) . Ertugliflozin (PF-04971729) is a potent, selective and orally active inhibitor of the sodium-dependent glucose cotransporter 2 (SGLT2), with an IC50 of 0.877 nM for h-SGLT2[1]. Has the potential for the treatment of type 2 diabetes mellitus[2].

Product Specifications

Product Name Alternative

PF-04971729-d9

UNSPSC

12352005

Target

Isotope-Labeled Compounds; SGLT

Type

Isotope-Labeled Compounds

Related Pathways

Membrane Transporter/Ion Channel; Others

Applications

Metabolism-sugar/lipid metabolism

Field of Research

Metabolic Disease

Solubility

10 mM in DMSO

Smiles

ClC1=CC=C([C@]23O[C@@](CO)(CO3)[C@@H](O)[C@H](O)[C@H]2O)C=C1CC4=C([2H])C([2H])=C(OC([2H])([2H])C([2H])([2H])[2H])C([2H])=C4[2H]

Molecular Formula

C22H16D9ClO7

Molecular Weight

445.94

References & Citations

[1]Mascitti V, et al. Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors. J Med Chem. 2011 Apr 28;54 (8) :2952-60.|[2]Miao Z, et al. Pharmacokinetics, metabolism, and excretion of the antidiabetic agent ertugliflozin (PF-04971729) in healthy male subjects. Drug Metab Dispos. 2013 Feb;41 (2) :445-56.|[3]Kalgutkar AS, et al. Preclinical species and human disposition of PF-04971729, a selective inhibitor of the sodium-dependent glucose cotransporter 2 and clinical candidate for the treatment of type 2 diabetes mellitus. Drug Metab Dispos. 2011 Sep;39 (9) :1609-19.|[4]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53 (2) :211-216.