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依格列净脯氨酸

依格列净脯氨酸用途

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。

依格列净脯氨酸名称

[ CAS 号 ]:
951382-34-6

[ 中文名 ]:
依格列净脯氨酸

[ 英文名 ]:
Ipragliflozin L-Proline

[中文别名 ]:

伊格列净L-脯氨酸盐

[英文别名 ]:

ASP-1941
Ipragliflozin L-proline
UNII-M6N3GK48A4
Ipragliflozin (L-Proline)

依格列净脯氨酸生物活性

[ 描述 ]:

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。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> SGLT

研究领域 >> 代谢疾病

[ 靶点 ]

IC50 value: 2.8 nM (SGLT2)[1][2].

[体外研究]

Ipragliflozin(L-Proline)在纳摩尔范围内有效且选择性地抑制人,大鼠和小鼠SGLT2,并显示出对抗肠葡萄糖苷酶的稳定性[3]。

[体内研究]

Ipragliflozin(L-Proline)在口服给药后显示出良好的药代动力学特性,并且剂量依赖性地增加尿糖排泄,其在正常小鼠中持续超过12小时[3]。口服ipragliflozin可以剂量依赖的方式增加尿糖排泄,这种作用在0.3 mg/kg或更高剂量时显着,持续时间超过12 h [4]。单次给予ipragliflozin剂量依赖性地增加尿糖排泄,降低血糖和血浆胰岛素水平,并改善葡萄糖耐受不良[5]。

[参考文献]

[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.

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