溶解性 | DMSO |
存贮条件 | 储存温度-20°C |
产品介绍 | PF-04971729(Ertugliflozin)是钠离子依赖的葡萄糖协同转运蛋白2(SGLT2)抑制剂。 |
生化机理 |
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 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. |
别名 | 1,6-脱水-1-C-[4-氯-3-[(4-乙氧基苯基)甲基]苯基]-5-C-(羟基甲基)-beta-L-艾杜糖;PF04971729;PF 04971729;Ertugliflozin;PF04971729;PF 04971729;1,6-Anhydro-1-C-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-5-C-(hydroxymethyl)-beta-L-idopyranose |