Ertugliflozin L-pyroglutamic acid

Modify Date: 2024-01-14 09:55:57

Ertugliflozin L-pyroglutamic acid Structure
Ertugliflozin L-pyroglutamic acid structure
Common Name Ertugliflozin L-pyroglutamic acid
CAS Number 1210344-83-4 Molecular Weight 565.997
Density N/A Boiling Point N/A
Molecular Formula C27H32ClNO10 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Ertugliflozin L-pyroglutamic acid


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].

 Names

Name Ertugliflozin L-pyroglutamic acid
Synonym More Synonyms

 Ertugliflozin L-pyroglutamic acid 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
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.

 Chemical & Physical Properties

Molecular Formula C27H32ClNO10
Molecular Weight 565.997
Exact Mass 565.171448
Storage condition 2-8℃

 Synonyms

MLU731K321