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Ipragliflozin
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Ipragliflozin图片
CAS NO:761423-87-4
包装与价格：
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
Ipragliflozin (ASP1941) 是一种具有口服活性的选择性 SGLT2 抑制剂，对人 SGLT2 和 SGLT1、大鼠 SGLT2 和 SGLT1、小鼠 SGLT2 和 SGLT1 的 IC50 分别为 7.38 和 1876 nM、6.73 和 1166 nM、5.64 和 1380 nM。
Cas No.761423-87-4
别名伊格列净; ASP1941
化学名(2S,3R,4R,5S,6R)-2-[3-(1-benzothiophen-2-ylmethyl)-4-fluorophenyl]-6-(hydroxymethyl)oxane-3,4,5-triol
Canonical SMILESC1=CC=C2C(=C1)C=C(S2)CC3=C(C=CC(=C3)C4C(C(C(C(O4)CO)O)O)O)F
分子式C21H21FO5S
分子量404.45
溶解度DMF: 30 mg/mL,DMSO: 30 mg/mL,Ethanol: 30 mg/mL,Ethanol:PBS (pH7.2) (1:7): 0.13 mg/mL
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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].

References:
[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.