Ertugliflozin-d5

Modify Date: 2024-01-11 05:48:32

Ertugliflozin-d5 Structure
Ertugliflozin-d5 structure
Common Name Ertugliflozin-d5
CAS Number 1298086-22-2 Molecular Weight 441.91
Density N/A Boiling Point N/A
Molecular Formula C22H20D5ClO7 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Ertugliflozin-d5


Ertugliflozin-d5 is the deuterium labeled Ertugliflozin[1]. Ertugliflozin (PF-04971729) 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[2]. Has the potential for the treatment of type 2 diabetes mellitus[3].

 Names

Name Ertugliflozin-d5

 Ertugliflozin-d5 Biological Activity

Description Ertugliflozin-d5 is the deuterium labeled Ertugliflozin[1]. Ertugliflozin (PF-04971729) 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[2]. Has the potential for the treatment of type 2 diabetes mellitus[3].
Related Catalog
In Vitro Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
References

[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216.  

[2]. 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.  

[3]. Miao Z, et al. Pharmacokinetics, metabolism, and excretion of the antidiabetic agent ertugliflozin (PF-04971729) in healthy male subjects. Drug Metab Dispos. 2013 Feb41(2):445-56.  

[4]. 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 Sep39(9):1609-19.  

 Chemical & Physical Properties

Molecular Formula C22H20D5ClO7
Molecular Weight 441.91