2. Membrane Transporter/Ion Channel
  3. SGLT
  4. Ipragliflozin

Ipragliflozin  (Synonyms: ASP1941)

Cat. No.: HY-14894 Purity: 99.78%
SDS COA Handling Instructions

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Ipragliflozin (ASP1941) is an orally active and selective SGLT2 inhibitor with IC50s 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.

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

Ipragliflozin Chemical Structure

Ipragliflozin Chemical Structure

CAS No. : 761423-87-4

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Based on 6 publication(s) in Google Scholar

Other Forms of Ipragliflozin:

Ipragliflozin Related Antibodies

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SGLT1 SGLT2

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Description

Ipragliflozin (ASP1941) is an orally active and selective SGLT2 inhibitor with IC50s 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[1]

hSGLT2

7.38 nM (IC50)

hSGLT1

1876 nM (IC50)

rSGLT2

6.73 nM (IC50)

rSGLT1

1166 nM (IC50)

mSGLT2

5.64 nM (IC50)

mSGLT1

1380 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
CHO IC50
7.4 nM
Compound: 14h, ASP1941, ipragliflozin
Inhibition of human SGLT2 expressed in CHO cells assessed as [14C]AMG accumulation after 2 hrs by scintillation counting
Inhibition of human SGLT2 expressed in CHO cells assessed as [14C]AMG accumulation after 2 hrs by scintillation counting
[PMID: 22507206]
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].

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

Ipragliflozin Related Antibodies

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-Ay 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].

MedChemExpress (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-Ay 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 HbA1c 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
Molecular Weight

404.45

Formula

C21H21FO5S
CAS No.
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (247.25 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

*"≥" 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.78%

SDS (252 KB)

COA (254 KB) LCMS (266 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4725 mL 12.3625 mL 24.7249 mL 61.8123 mL
5 mM 0.4945 mL 2.4725 mL 4.9450 mL 12.3625 mL
10 mM 0.2472 mL 1.2362 mL 2.4725 mL 6.1812 mL
15 mM 0.1648 mL 0.8242 mL 1.6483 mL 4.1208 mL
20 mM 0.1236 mL 0.6181 mL 1.2362 mL 3.0906 mL
25 mM 0.0989 mL 0.4945 mL 0.9890 mL 2.4725 mL
30 mM 0.0824 mL 0.4121 mL 0.8242 mL 2.0604 mL
40 mM 0.0618 mL 0.3091 mL 0.6181 mL 1.5453 mL
50 mM 0.0494 mL 0.2472 mL 0.4945 mL 1.2362 mL
60 mM 0.0412 mL 0.2060 mL 0.4121 mL 1.0302 mL
80 mM 0.0309 mL 0.1545 mL 0.3091 mL 0.7727 mL
100 mM 0.0247 mL 0.1236 mL 0.2472 mL 0.6181 mL
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Ipragliflozin Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Ipragliflozin761423-87-4ASP1941ASP 1941ASP-1941SGLTSodium-dependent glucose cotransportersInhibitorinhibitorinhibit

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