Ertugliflozin L-pyroglutamic acid

Ertugliflozin L-pyroglutamic acid (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]. Has the potential for the treatment of type 2 diabetes mellitus[2].

Product Specifications

CAS Number

[1210344-83-4]

Product Name Alternative

PF-04971729 L-pyroglutamic acid

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

SGLT

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel

Applications

Metabolism-sugar/lipid metabolism

Field of Research

Metabolic Disease

Assay Protocol

https://www.medchemexpress.com/Ertugliflozin_L-pyroglutamic_acid.html

Concentration

10mM

Purity

99.84

Solubility

DMSO : 100 mg/mL (ultrasonic) |H2O : 5 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

ClC1=CC=C([C@]23O[C@@](CO)(CO3)[C@@H](O)[C@H](O)[C@H]2O)C=C1CC4=CC=C(OCC)C=C4.O=C5CC[C@@H](C(O)=O)N5

Molecular Formula

C27H32ClNO10

Molecular Weight

566.00

Precautions

H302, H315, H319, H335

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.