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Ertugliflozin

Names

[ CAS No. ]:
1210344-57-2

[ Name ]:
Ertugliflozin

[Synonym ]:
(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

Biological Activity

[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.


[Related Small Molecules]

Phlorizin | Phloretin | LX-4211 | Licogliflozin | Tofogliflozin (hydrate) | Bexagliflozin | Ipragliflozin | Ertugliflozin L-pyroglutamic acid | Velagliflozin

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Boiling Point ]:
630.5±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C22H25ClO7

[ Molecular Weight ]:
436.883

[ Flash Point ]:
335.1±31.5 °C

[ Exact Mass ]:
436.128876

[ PSA ]:
108.61000

[ LogP ]:
6.49

[ Vapour Pressure ]:
0.0±1.9 mmHg at 25°C

[ Index of Refraction ]:
1.652

[ Storage condition ]:
-20℃

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Related Compounds