1210344-83-4

1210344-83-4 structure

Name: Ertugliflozin L-pyroglutamic acid
Chemical Name: Ertugliflozin L-pyroglutamic acid
CAS Number: 1210344-83-4
Molecular Formula: C₂₇H₃₂ClNO₁₀
Molecular Weight: 565.997
Catalog: Signaling Pathways Membrane Transporter/Ion Channel SGLT
Create Date: 2018-07-20 02:15:48
Modify Date: 2024-01-14 09:55:57
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].

Name	Ertugliflozin L-pyroglutamic acid
Synonyms	MLU731K321

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.