伊格列净

更新时间：2025-08-20 09:49:03

伊格列净结构式	常用名	伊格列净	英文名	Ipragliflozin
	CAS号	761423-87-4	分子量	404.452
	密度	1.5±0.1 g/cm3	沸点	628.8±55.0 °C at 760 mmHg
	分子式	C₂₁H₂₁FO₅S	熔点	N/A
	MSDS	N/A	闪点	334.1±31.5 °C

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。

中文名	伊格列净
英文名	(2S,3R,4R,5S,6R)-2-[3-(1-benzothiophen-2-ylmethyl)-4-fluorophenyl]-6-(hydroxymethyl)oxane-3,4,5-triol
英文别名	更多

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.

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.

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
InChIKey	AHFWIQIYAXSLBA-RQXATKFSSA-N
SMILES	OCC1OC(c2ccc(F)c(Cc3cc4ccccc4s3)c2)C(O)C(O)C1O
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℃

(1S)-1,5-anhydr...

761423-01-2

~88%

伊格列净

761423-87-4

文献：Astellas Pharma Inc.; Kotobuki Pharmaceutical Co., Ltd. Patent: EP2105442 A1, 2009 ; Location in patent: Page/Page column 13 ;

(1S)-1,5-脱水-1-C...

1034305-21-9

~97%

伊格列净

761423-87-4

文献：Astellas Pharma Inc.; Kotobuki Pharmaceutical Co., Ltd. Patent: EP2105442 A1, 2009 ; Location in patent: Page/Page column 15 ;

苯并[B]噻吩-2-基(5-溴...

1034305-11-7

伊格列净

761423-87-4

文献：Bioorganic and Medicinal Chemistry, , vol. 20, # 10 p. 3263 - 3279

2-(5-溴-2-氟苄基)苯并噻吩

1034305-17-3

伊格列净

761423-87-4

文献：Bioorganic and Medicinal Chemistry, , vol. 20, # 10 p. 3263 - 3279

5-溴-2-氟苯甲醛

93777-26-5

伊格列净

761423-87-4

文献：Bioorganic and Medicinal Chemistry, , vol. 20, # 10 p. 3263 - 3279

苯并噻吩

95-15-8

伊格列净

761423-87-4

文献：Bioorganic and Medicinal Chemistry, , vol. 20, # 10 p. 3263 - 3279

伊格列净上游产品 5
CAS号1034305-21-9 (1S)-1,5-脱水-1-C... CAS号1034305-11-7 苯并[B]噻吩-2-基(5-溴... CAS号1034305-17-3 2-(5-溴-2-氟苄基)苯并噻吩 CAS号93777-26-5 5-溴-2-氟苯甲醛
CAS号95-15-8 苯并噻吩
伊格列净下游产品 0

实验名称：Binding affinity towards rat Gabra1 in an in vitro assay with cellular components mea...
来源：ChEMBL
靶标：Gamma-aminobutyric acid receptor subunit alpha-1
External Id：CHEMBL5291800

实验名称：Inhibition of SGLT2 (unknown origin)
来源：ChEMBL
靶标：Sodium/glucose cotransporter 2
External Id：CHEMBL4344293

实验名称：Human Sodium/glucose cotransporter 2 (Hexose transporter family)
来源：IUPHAR-DB
靶标：Sodium/glucose cotransporter 2 (Hexose transporter family) [Homo sapiens]
External Id：916_Human

实验名称：Inhibition of SGLT1 (unknown origin)
来源：ChEMBL
靶标：Sodium/glucose cotransporter 1
External Id：CHEMBL4344292

实验名称：Binding affinity towards human ESR1 in an in vitro cell free assay (CRO assay) measur...
来源：ChEMBL
靶标：Estrogen receptor
External Id：CHEMBL5291792

实验名称：Compound was evaluated for inhibition of human F2 in an in vitro cell free assay meas...
来源：ChEMBL
靶标：Prothrombin
External Id：CHEMBL5291794

实验名称：Cytotoxicity counterscreen for inhibitors of SARS-CoV-2 cell entry
来源：NCGC
靶标：N/A
External Id：TRND-SARS-CoV-2-cytotox-48hr

实验名称：Primary qHTS to identify inhibitors of SARS-CoV-2 cell entry
来源：NCGC
External Id：TRND-SARS-CoV-2-PP

实验名称：Human Sodium/glucose cotransporter 1 (Hexose transporter family)
来源：IUPHAR-DB
靶标：Sodium/glucose cotransporter 1 (Hexose transporter family) [Homo sapiens]
External Id：915_Human

实验名称：Binding affinity towards human DRD1 in an in vitro assay with cellular components (NI...
来源：ChEMBL
靶标：D(1A) dopamine receptor
External Id：CHEMBL5291779

共71条，当前第1页，共8页

ASP1941

UNII-3N2N8OOR7X

ASP 1941

(1S)-1,5-Anhydro-1-[3-(1-benzothiophen-2-ylmethyl)-4-fluorophenyl]-D-glucitol

Suglat

Ipragliflozin

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

伊格列净合成线路

伊格列净上下游产品

伊格列净靶点实验

伊格列净英文别名

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