Mizagliflozin (Synonyms: DSP-3235 free base; KGA-3235 free base; GSK-1614235 free base) |
| カタログ番号GC60249 |
ミザグリフロジン (DSP-3235 遊離塩基) は、ヒト SGLT1 に対して 27 nM の Ki を持つ、強力な経口活性の選択的 SGLT1 阻害剤です。
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Cas No.: 666843-10-3
Sample solution is provided at 25 µL, 10mM.
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Mizagliflozin (DSP-3235 free base) is a potent, orally active and selective SGLT1 inhibitor, with a Ki of 27 nM for human SGLT1. Mizagliflozin displays 303-fold selectivity over SGLT2. Mizagliflozin is used as an antidiabetic drug that can modify postprandial blood glucose excursion. Mizagliflozin also exhibits potential in the amelioration of chronic constipation[1].
Mizagliflozin (DSP-3235 free base) (3-30 mg/kg; oral) exerts a laxative effect[1].Mizagliflozin administrated intravenously (0.3 mg/kg) and orally (3 mg/kg) declined with a short half-life (0.23 and 1.14 h, respectively)[2] Animal Model: Male Wistar rats (rat model of low-fiber-diet-induced constipation)[1]
[1]. Inoue T, et al. Mizagliflozin, a novel selective SGLT1 inhibitor, exhibits potential in the amelioration of chronic constipation. Eur J Pharmacol. 2017 Jul 5;806:25-31. [2]. Ohno H, et al. Absorption, disposition, metabolism and excretion of [14C]mizagliflozin, a novel selective SGLT1 inhibitor, in rats. Xenobiotica. 2019 Apr;49(4):463-473.
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