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伊格列净

伊格列净用途

Ipragliflozin (ASP1941)是高活性SGLT2选择性抑制剂,IC50为2.8 nM,对SGLT1/3/4/5/6几乎无活性。

伊格列净名称

[ CAS 号 ]:
761423-87-4

[ 中文名 ]:
伊格列净

[ 英文名 ]:
Ipragliflozin

[英文别名 ]:

ASP1941
UNII-3N2N8OOR7X
ASP 1941
Suglat
Ipragliflozin

伊格列净生物活性

[ 描述 ]:

Ipragliflozin (ASP1941)是高活性SGLT2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

[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.

[6]. Yoshikawa T, et al. Arterial pressure lability is improved by sodium-glucose cotransporter 2 inhibitor in streptozotocin-induced diabetic rats. Hypertens Res. 2017 Jul;40(7):646-651.

[7]. Sakaeda T, et al. Susceptibility to serious skin and subcutaneous tissue disorders and skin tissue distribution of sodium-dependent glucose co-transporter type 2 (SGLT2) inhibitors. Int J Med Sci. 2018 Jun 13;15(9):937-943.

[相关活性小分子]

伊格列净物理化学性质

[ 密度 ]:
1.5±0.1 g/cm3

[ 沸点 ]:
628.8±55.0 °C at 760 mmHg

[ 分子式 ]:
C₂₁H₂₁FO₅S

[ 分子量 ]:
404.452

[ 闪点 ]:
334.1±31.5 °C

[ 精确质量 ]:
404.109375

[ PSA ]:
118.39000

[ LogP ]:
5.59

[ 外观性状 ]:
粉末

[ 蒸汽压 ]:
0.0±1.9 mmHg at 25°C

[ 折射率 ]:
1.684

[ 储存条件 ]:
-20℃

伊格列净

伊格列净用途

伊格列净名称

伊格列净生物活性

伊格列净物理化学性质

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