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[CAS NO. 761423-87-4] Ipragliflozin

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Catalog:	HY-14894
Brand:	MCE
CAS:	761423-87-4

Overview

MDL	MFCD19443744
Molecular Weight	404.45
Molecular Formula	C21H21FO5S
SMILES	FC1=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

For research use only. We do not sell to patients.

5 Publications Citing Use of MCE

[1]Biochem Pharmacol. 2018 Jun;152:45-59.
[2]Biochem Pharmacol. 2016 Feb 1;101:27-39.
[3]J Chromatogr B Analyt Technol Biomed Life Sci. 2015 Sep 1;1000:22-8.
[4]Hypertens Res. 2017 Jul;40(7):646-651.
[5]Int J Med Sci. 2018 Jun 13;15(9):937-943.

Summary

Ipragliflozin (ASP1941) is an orally active and selective SGLT2 inhibitor with IC ₅₀ s of 7.38 and 1876 nM, 6.73 and 1166 nM, 5.64 and 1380 nM for human SGLT2 and SGLT1 , rat SGLT2 and SGLT1 , mouse SGLT2 and SGLT1 , respectively. Antidiabetic agent ^[1] .

IC50 & Target

hSGLT2

7.38 nM (IC ₅₀ )

hSGLT1

1876 nM (IC ₅₀ )

rSGLT2

6.73 nM (IC ₅₀ )

rSGLT1

1166 nM (IC ₅₀ )

mSGLT2

5.64 nM (IC ₅₀ )

mSGLT1

1380 nM (IC ₅₀ )

In Vitro

Ipragliflozin (1-50 μM) significantly and dose-dependently suppresses the growth of MCF-7 human breast cancer cell lines.
Upon knocking down SGLT2 expression using siRNA, the attenuation of cell proliferation induced by Ipragliflozin is completely canceled, suggesting that Ipragliflozin attenuates breast cancer cell proliferation through SGLT2 inhibition.
BrdU assay revealed that Ipragliflozin at a high dose (50 and 100 μM) significantly inhibits DNA synthesis of MCF-7 cells ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay ^[2]

Cell Line:	MCF-7 human breast cancer cell lines
Concentration:	1, 10, 50 μM
Incubation Time:	24, 48, 72, 96 hours
Result:	Decreased the number of MCF-7 cells in a dose-dependent manner.

In Vivo

Ipragliflozin shows antihyperglycemic effect. Ipragliflozin (0.1-1 mg/kg) dose-dependently inhibits increases in blood glucose levels. In STZ-induced type 1 diabetic rats, this effect is significant at doses of 0.3 and 1 mg/kg, and in KK-A ^y type 2 diabetic mice, the effect is significant at all tested doses ^[1] .
Ipragliflozin (0.3 and 1 mg/kg) shows antidiabetic effects of repeated administration in streptozotocin-induced type 1 diabetic rats ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Single Administration ^[1] Streptozotocin (STZ; 50 mg/kg)-induced type 1 diabetic rats and KK-A ^y type 2 diabetic mice
Dosage:	0.1-1 mg/kg
Administration:	Single oral administration in the fed condition. Blood glucose levels were then measured for 8 h under fasting conditions.
Result:	Dose-dependently lowered blood glucose levels, and this effect was significant at all tested doses.

Animal Model:	Repeated Administration ^[1] Streptozotocin (STZ; 50 mg/kg)-induced type 1 diabetic rats
Dosage:	0.3 and 1 mg/kg
Administration:	Administration orally once daily (at night) for 4 weeks.
Result:	Significantly reduced the levels of HbA _1c and blood glucose. Pancreatic insulin content was significantly increased at a dose of 1 mg/kg. Urinary glucose excretion was increased dose-dependently, and this was significant at the 1 mg/kg dose.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT01403818	Astellas Pharma Inc	Healthy\|Pharmacokinetics of ASP1941\|Pharmacokinetics of Mitiglinide	June 2011	Phase 1
NCT01674777	Astellas Pharma Inc	Healthy\|Pharmacokinetics of ASP1941	October 2010	Phase 1
NCT02897219	Astellas Pharma Inc	Type 1 Diabetes Mellitus	August 29, 2016	Phase 3
NCT01316094	Astellas Pharma Inc	Type 2 Diabetes Mellitus	January 18, 2011	Phase 3
NCT02175784	Astellas Pharma Inc	Type 2 Diabetes Mellitus	March 31, 2014	Phase 4
NCT02847091	Astellas Pharma Inc	Type 2 Diabetes Mellitus	July 29, 2016	Phase 4
NCT02564211	Merck Sharp & Dohme LLC	Type 2 Diabetes Mellitus	October 26, 2015	Phase 3
NCT01514838	Astellas Pharma Inc	Type II Diabetes Mellitus	April 23, 2012	Phase 3
NCT01288898	Astellas Pharma Inc	Healthy	May 2007	Phase 1
NCT01088919	Astellas Pharma Inc	Healthy\|Pharmacokinetics of ASP1941	November 2009	Phase 1
NCT01242202	Astellas Pharma Inc	Type 2 Diabetes Mellitus	October 21, 2010	Phase 3
NCT02529449	Astellas Pharma Inc	Type 1 Diabetes Mellitus	September 1, 2015	Phase 2
NCT01023945	Astellas Pharma Inc	Type 2 Diabetes Mellitus	November 7, 2009	Phase 1
NCT00621868	Astellas Pharma Inc	Diabetes Mellitus	March 26, 2008	Phase 2
NCT01302132	Astellas Pharma Inc	Healthy Subjects	May 2008	Phase 1
NCT01071850	Astellas Pharma Inc	Diabetes Mellitus, Type 2	March 3, 2010	Phase 2
NCT01187186	Astellas Pharma Inc	Liver Disease	May 2010	Phase 1
NCT00790660	Astellas Pharma Inc	Diabetes Mellitus, Type 2	October 23, 2008	Phase 2
NCT01242228	Astellas Pharma Inc	Type 2 Diabetes Mellitus	October 21, 2010	Phase 3
NCT01972880	Astellas Pharma Inc	Healthy\|Plasma Concentration of ASP1941	September 2013	Phase 1
NCT01672762	Astellas Pharma Inc	Type 2 Diabetes Mellitus	May 25, 2012	Phase 3
NCT01302145	Astellas Pharma Inc	Type 2 Diabetes Mellitus	February 25, 2009	Phase 1
NCT01057628	Astellas Pharma Inc	Type 2 Diabetes Mellitus	January 13, 2010	Phase 3
NCT01316107	Astellas Pharma Inc	Type 2 Diabetes Mellitus	January 15, 2011	Phase 3
NCT01242215	Astellas Pharma Inc	Type 2 Diabetes Mellitus	September 17, 2010	Phase 3
NCT02452632	Astellas Pharma Korea, Inc.\|Astellas Pharma Inc	Type 2 Diabetes Mellitus	June 22, 2015	Phase 3
NCT01099839	Astellas Pharma Inc	Healthy Volunteers\|Pharmacokinetics of ASP1941	February 2010	Phase 1
NCT01302028	Astellas Pharma Inc	Type 2 Diabetes Mellitus	January 22, 2010	Phase 1
NCT01121198	Astellas Pharma Inc	Healthy Volunteer\|Pharmacokinetics of ASP1941	December 2006	Phase 1
NCT02875821	Yonsei University	Type 2 Diabetes With Non-alcoholic Fatty Liver (NAFLD)	April 26, 2016	Phase 4
NCT02794792	Astellas Pharma Europe B.V.\|Astellas Pharma Inc	Type 2 Diabetes Mellitus	May 11, 2016	Phase 3
NCT02791035	Asan Medical Center\|Severance Hospital\|Samsung Medical Center\|Kyung Hee University Hospital at Gangdong\|Astellas Pharma Korea, Inc.	Type 2 Diabetes Mellitus	June 2016	Phase 4
NCT01611428	Astellas Pharma Europe B.V.\|Astellas Pharma Inc	Bioavailability of Ipragliflozin\|Healthy Subjects	June 2011	Phase 1
NCT01302158	Astellas Pharma Inc	Healthy Subjects	December 2009	Phase 1
NCT01117584	Astellas Pharma Inc	Type 2 Diabetes Mellitus	April 6, 2010	Phase 2
NCT01054092	Astellas Pharma Inc	Type 2 Diabetes Mellitus	January 14, 2010	Phase 3
NCT01135433	Astellas Pharma Inc	Type 2 Diabetes Mellitus	May 15, 2010	Phase 3
NCT01611415	Astellas Pharma Europe B.V.\|Astellas Pharma Inc	Healthy Subjects\|Pharmacokinetics of Ipragliflozin	July 2011	Phase 1
NCT02317484	Translational Research Center for Medical Innovation, Kobe, Hyogo, Japan\|Osaka Saiseikai Nakatsu Hospital\|Astellas Pharma Inc	Diabetes Mellitus, Type 2	November 2014
NCT02577003	Merck Sharp & Dohme LLC	Type 2 Diabetes Mellitus	November 9, 2015	Phase 3
NCT01373060	Astellas Pharma Inc\|Astellas Pharma Taiwan, Inc.	Healthy\|Pharmacokinetics of ASP1941	February 2011	Phase 1
NCT01505426	Astellas Pharma Inc	Type II Diabetes Mellitus	November 28, 2011	Phase 3
NCT01678287	Astellas Pharma Global Development, Inc.\|Astellas Pharma Inc	Healthy Volunteers\|Pharmacokinetics of ASP1941	November 2007	Phase 1
NCT01232413	Astellas Pharma Inc	Healthy Subjects\|Cardiac Repolarization	September 2010	Phase 1
NCT01104532	Astellas Pharma Inc	Healthy\|Pharmacokinetics of ASP1941	February 2010	Phase 1
NCT01611363	Astellas Pharma Europe B.V.\|Astellas Pharma Inc	Type 2 Diabetes Mellitus	October 27, 2011	Phase 1
NCT01288885	Astellas Pharma Inc	Healthy	November 2006	Phase 1
NCT02479399	Astellas Pharma Inc	Type 2 Diabetes	July 17, 2014
NCT03076112	Seoul National University Bundang Hospital\|Astellas Pharma Korea, Inc.	Type 2 Diabetes Mellitus	April 25, 2017	Phase 3
NCT01225081	Astellas Pharma Inc	Type 2 Diabetes Mellitus	September 15, 2010	Phase 3
NCT02577016	Merck Sharp & Dohme LLC	Type 2 Diabetes Mellitus	November 5, 2015	Phase 3
NCT03118713	Astellas Pharma Korea, Inc.\|Astellas Pharma Inc	Type 2 Diabetes Mellitus	April 25, 2017	Phase 4
NCT01097681	Astellas Pharma Inc	Type 2 Diabetes Mellitus	February 16, 2010	Phase 1
NCT02291874	Astellas Pharma Inc	Type 2 Diabetes Mellitus	October 8, 2014	Phase 4

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL ( 247.25 mM )

H ₂ O : ≥ 0.1 mg/mL ( 0.25 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.4725 mL	12.3625 mL	24.7249 mL
5 mM	0.4945 mL	2.4725 mL	4.9450 mL
10 mM	0.2472 mL	1.2362 mL	2.4725 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (6.18 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (6.18 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (6.18 mM); Clear solution

* All of the co-solvents are available by MCE.

References

[1] Atsuo Tahara, 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.
[2] Shiho Komatsu, et al. SGLT2 inhibitor ipragliflozin attenuates breast cancer cell proliferation. Endocr J. 2020 Jan 28;67(1):99-106.

Synonyms

D-Glucitol, 1,5-anhydro-1-C-[3-(benzo[b]thien-2-ylmethyl)-4-fluorophenyl]-, (1S)-

(1S)-1,5-Anhydro-1-C-[3-(benzo[b]thien-2-ylmethyl)-4-fluorophenyl]-D-glucitol

Ipragliflozin

ASP 1941

Suglat

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