Ertugliflozin PF-04971729;Ertugliflozin;Ertugliflozin/PF-04971729;PF-04971729/PF04971729;1,6-Anhydro-1-C-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-5-C-(hydroxymethyl)-beta-L-idopyranose;PF 04971729-00;PF-04971729 1210344-57-2
PF-04971729(Ertugliflozin) is a potent and selective inhibitor of the sodium-dependent glucose cotransporter 2(SGLT2).
IC50 value:
Target: SGLT2
PF-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 a Tmax at ~ 1.0 h. Of the total radioactivity excreted in feces and urine, unchanged PF-04971729 collectively accounted for ~ 35.3% of the dose, suggestive of moderate metabolic elimination in humans.
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