PF-04971729_1210344-57-2_DataSheet_MedChemExpress
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Product Name:
PF-04971729CAS No.:
1210344-57-2Cat. No.:
HY-15461Product Data Sheet
MWt:
436.88Formula:
C22H25ClO7Purity :>98%
Solubility:
DMSO
Mechanisms:
Biological Activity:
PF-04971729(Ertugliflozin)is a potent and selective inhibitor of the sodium-dependent glucose Pathways:Membrane Tranporter/Ion Channel; Target:SGLT PF-04971729(Ertugliflozin) is a potent and selective inhibitor of the sodium-dependent glucose
cotransporter 2(SGLT2).
IC50 value:
Target: SGLT2PF-04971729 is currently in phase 2 trials for the treatment of diabetes mellitus. Inhibitory effects against the organic cation transporter 2-mediated uptake of [14C]metformin by PF-04971729 also were very weak (IC50 900μM).The disposition of PF-04971729, an orally active selective inhibitor of the sodium-dependent glucose cotransporter 2, was studied after a single 25-mg oral dose of [14C]-PF-04971729 to healthy human subjects. The absorption of PF-04971729 in humans was rapid with 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.a Tmax at ~ 1.0 h. Of the total radioactivity excreted in feces and urine, unchanged PF-04971729collectively accounted for ~ 35.3% of the dose, suggestive of moderate metabolic elimination in humans....
p ;()[2]. 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.[3]. 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.Caution: Not fully tested. For research purposes only
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