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[CAS NO. 761423-87-4]  Ipragliflozin

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PRODUCTS SPECIFICATIONS [761423-87-4]

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

DESCRIPTION [761423-87-4]

Overview

MDLMFCD19443744
Molecular Weight404.45
Molecular FormulaC21H21FO5S
SMILESFC1=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


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

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.


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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