1210344-57-2

1210344-57-2 structure

Name: Ertugliflozin
Chemical Name: (1S,2S,3S,4R,5S)-5-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-1-(hydroxymethyl)-6,8-dioxabicyclo[3.2.1]octane-2,3,4-triol
CAS Number: 1210344-57-2
Molecular Formula: C₂₂H₂₅ClO₇
Molecular Weight: 436.883
Catalog: API Hormone and endocrine-regulating drugs Pancreatic hormones and other blood sugar regulating drugs
Create Date: 2018-05-14 08:00:00
Modify Date: 2024-01-02 20:30:06
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[1]. A drug for the treatment of type 2 diabetes mellitus[2].

Name	(1S,2S,3S,4R,5S)-5-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-1-(hydroxymethyl)-6,8-dioxabicyclo[3.2.1]octane-2,3,4-triol
Synonyms	(1S,2S,3S,4R,5S)-5-[4-Chloro-3-(4-ethoxybenzyl)phenyl]-1-(hydroxymethyl)-6,8-dioxabicyclo[3.2.1]octane-2,3,4-triol Ertugliflozin PF-04971729 Ertugliflozin (USAN/INN) PF-04971729-00 MK-8835 cc-212 (1S,2S,3S,4R,5S)-5-[4-chloro-3-(4-ethoxybenzyl)phenyl]-1-hydroxymethyl-6,8-dioxabicyclo[3.2.1]octane-2,3,4-triol

Description	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[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.

1210763-25-9

~28%

1210344-57-2

1210344-58-3

Literature: WO2010/23594 A1, ; Page/Page column 64-66 ;

1233482-00-2

1210344-57-2

Literature: Organic Letters, , vol. 12, # 13 p. 2940 - 2943

Precursor 2
1210763-25-9 1233482-00-2
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