CAS 1210344-83-4|Ertugliflozin L-pyroglutamic acid

Introduction:Basic information about CAS 1210344-83-4|Ertugliflozin L-pyroglutamic acid, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
Common NameErtugliflozin L-pyroglutamic acid
CAS Number1210344-83-4Molecular Weight565.997
Density/Boiling Point/
Molecular FormulaC27H32ClNO10Melting Point/
MSDS/Flash Point/

Names

NameErtugliflozin L-pyroglutamic acid
SynonymMore Synonyms

Ertugliflozin L-pyroglutamic acid BiologicalActivity

DescriptionErtugliflozin (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 CatalogSignaling Pathways >>Membrane Transporter/Ion Channel >>SGLTResearch Areas >>Metabolic Disease
Target

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

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

Chemical & Physical Properties

Molecular FormulaC27H32ClNO10
Molecular Weight565.997
Exact Mass565.171448
Storage condition2-8℃

Synonyms

MLU731K321
CAS 1196703-48-6|Fmoc-Phe-Thr(psi(Me,Me)pro)-OH
CAS 12237-27-3|N-Ethyl-N-methyl-3-(3-pyrrolidinyl)benzamide hydrochloride (1:1)
Recommended......
TOP