Ertugliflozin L-pyroglutamic acid

Names

[ Name ]:
Ertugliflozin L-pyroglutamic acid

[Synonym ]:
MLU731K321

Biological Activity

[Description]:

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].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> SGLT

Research Areas >> Metabolic Disease

[Target]

IC50: 0.877 nM (h-SGLT2)[1].

[In Vitro]

Ertugliflozin (PF-04971729) demonstrates >2000-fold selectivity for SGLT2 inhibition (relative to SGLT1) in vitro[3].

[In Vivo]

Ertugliflozin (PF-04971729) reveals a concentration-dependent glucosuria after oral administration to rats[3].

[References]

[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.

[Related Small Molecules]

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₇H₃₂ClNO₁₀

[ Molecular Weight ]:
565.997

[ Exact Mass ]:
565.171448

[ Storage condition ]:
2-8℃

Ertugliflozin L-pyroglutamic acid

Names

Biological Activity

Chemical & Physical Properties

Related Compounds