Ertugliflozin L-pyroglutamic acid |
| Catalog No.GC36004 |
L'acide L-pyroglutamique d'ertugliflozine (acide L-pyroglutamique PF-04971729) est un inhibiteur puissant, sélectif et actif par voie orale du cotransporteur de glucose dépendant du sodium 2 (SGLT2), avec une IC50 de 0,877 nM pour h-SGLT2.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1210344-83-4
Sample solution is provided at 25 µL, 10mM.
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Ertugliflozin (PF-04971729) L-pyroglutamic acid 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]. A drug for the treatment of type 2 diabetes mellitus[2]. IC50: 0.877 nM (h-SGLT2)[1].
Ertugliflozin (PF-04971729) demonstrates >2000-fold selectivity for SGLT2 inhibition (relative to SGLT1) in vitro[3].
Ertugliflozin (PF-04971729) reveals a concentration-dependent glucosuria after oral administration to rats[3].
[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.
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