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Ipragliflozin L-Proline
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 L-Proline图片
CAS NO:951382-34-6
包装与价格：
包装价格(元)
5mg电议
10mg电议
50mg电议

产品介绍
Ipragliflozin (L-Proline) 是 SGLT2 高活性的，选择性抑制剂，IC50 为 2.8 nM，对 SGLT1/3/4/5/6 几乎无活性。
Cas No.951382-34-6
别名L-脯氨酸与(1S)-1,5-脱水-1-C-[3-(苯并[B]噻吩-2-基甲基)-4-氟苯基]-D-山梨糖醇的化合物
Canonical SMILESFC1=CC=C([C@H]2[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O2)C=C1CC3=CC(C=CC=C4)=C4S3.O=C(O)[C@H]5NCCC5
分子式C26H30FNO7S
分子量519.58
溶解度Soluble in DMSO
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 (L-Proline) is a highly potent and selective SGLT2 inhibitor with an IC50 of 2.8 nM; little and NO potency for SGLT1/3/4/5/6. IC50 value: 2.8 nM (SGLT2)[1][2].

Ipragliflozin (L-Proline) potently and selectively inhibits human, rat, and mouse SGLT2 at nanomolar ranges and exhibits stability against intestinal glucosidases[3].

Ipragliflozin (L-Proline) shows good pharmacokinetic properties following oral dosing, and dose-dependently increases urinary glucose excretion, which lasts for over 12 h in normal mice [3]. Oral administration of ipragliflozin increases urinary glucose excretion in a dose-dependent manner, an effect which is significant at doses of 0.3 mg/kg or higher and lasts over 12 h[4]. Single administration of ipragliflozin dose-dependently increases urinary glucose excretion, reduces blood glucose and plasma insulin levels, and improves glucose intolerance [5].

[1]. Imamura M, et al. Discovery of Ipragliflozin (ASP1941): a novel C-glucoside with benzothiophene structure as a potent and selective sodium glucose co-transporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes mellitus. Bioorg Med Chem. 2012 May 15;20(10):3263-79. [2]. Suzuki M, et al. Tofogliflozin, a potent and highly specific sodium/glucose cotransporter 2 inhibitor, improves glycemic control in diabetic rats and mice. J Pharmacol Exp Ther. 2012 Jun;341(3):692-701. [3]. Tahara A, et al. 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. [4]. Tahara A, et al. Antidiabetic effects of SGLT2-selective inhibitor ipragliflozin in streptozotocin-nicotinamide-induced mildly diabetic mice. J Pharmacol Sci. 2012;120(1):36-44. [5]. Tahara A, et al. Effects of SGLT2 selective inhibitor ipragliflozin on hyperglycemia, hyperlipidemia, hepatic steatosis, oxidative stress, inflammation, and obesity in type 2 diabetic mice. Eur J Pharmacol. 2013 Sep 5;715(1-3):246-55.