PF-04971729, a potent and selective inhibitor of the sodium-dependent glucose cotransporter 2, is currently in phase 2 trials for the treatment of diabetes mellitus. Inhibitory effects against the organic cation transporter 2-mediated upt
Storage Temp
Store at -20°C,Argon charged
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Sodium/glucose cotransporter 2 inhibitor
Product Description
PF-04971729(Ertugliflozin) is a potent and selective inhibitor of the sodium-dependent glucose cotransporter 2(SGLT2).
Ertugliflozin (MK-8835, PF-04971729) is a potent and selective sodium-dependent glucose cotransporter 2 inhibitor with IC50 values of 0.877 nM for h-SGLT2 and 1000-fold higher for h-SGLT1.
Product Properties
ALogP
1.7
Associated Targets(Human)
SLC5A4TchemSolute carrier family 5 member 4 (1 Activities)
1.Bays H. (2009) From victim to ally: the kidney as an emerging target for the treatment of diabetes mellitus.. Curr Med Res Opin, 25 (3):(671-81). [PMID:19232040][10.1021/op500134e]
2.Nair S, Wilding JP. (2010) Sodium glucose cotransporter 2 inhibitors as a new treatment for diabetes mellitus.. J Clin Endocrinol Metab, 95 (1):(34-42). [PMID:19892839][10.1021/op500134e]
3.Mascitti V, Maurer TS, Robinson RP, Bian J, Boustany-Kari CM, Brandt T, Collman BM, Kalgutkar AS, Klenotic MK, Leininger MT et al.. (2011) 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, 54 (8):(2952-60). [PMID:21449606][10.1021/op500134e]
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A2219484