An SGLT2 inhibitor
Ipragliflozin is a selective inhibitor of sodium–glucose cotransporter 2 (SGLT2) with IC50 value of 7.38nM [1].
Ipragliflozin is a derivative of phlorizin. It shows inhibition activity for mouse, rat and human SGLT2 with IC50 values of 7.38nM, 6.73nM and 5.64nM, respectively. It is not effective for SGLT1 with IC50 value of 1876nM. In the radioligand binding and enzyme assays, lpragliflozin shows no interaction with other receptors, channels, and transporters like adrenergic, muscarinic and calcium channel, demonstrating a specific inhibition of SGLT2. As a glucitol compound, ipragliflozin is stable against glucosidases in mouse small intestine [1].
Since SGLT2 plays a critical role in renal glucose reabsorption, ipragliflozin is therapeutic potent to treat hyperglycemia in diabetes through increasing glucose excretion into urine. In STZ-induced type 1 diabetic rats and KK-Ay type 2 diabetic mice, the single administration of ipragliflozin significantly decreases the blood glucose levels [1].
参考文献:
[1] Tahara A, Kurosaki E, Yokono M, Yamajuku D, Kihara R, Hayashizaki Y, Takasu T, Imamura M, Qun L, Tomiyama H, Kobayashi Y, Noda A, Sasamata M, Shibasaki M. Pharmacological profile of ipragliflozin (ASP1941), a novel selective SGLT2 inhibitor, in vitro and in vivo. Naunyn Schmiedebergs Arch Pharmacol. 2012 Apr;385(4):423-36.
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