Mizagliflozin (KWA 0711)

Catalog No.S8939 Batch:S893901

Technical Data

Formula

C₂₈H₄₄N₄O₈

Molecular Weight

564.67

CAS No.

666843-10-3

Solubility (25°C)*

In vitro

DMSO

100 mg/mL (177.09 mM)

Water

100 mg/mL (177.09 mM)

Ethanol

100 mg/mL (177.09 mM)

In vivo (Add solvents to the product individually and in order)

Clear solution	5% DMSO 1 95% Corn oil	0.83mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 16.6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	5.0mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

Mizagliflozin (KWA 0711) is a novel, potent, selective sodium glucose co-transporter 1 (SGLT1) inhibitor with Ki of 27 nM for human SGLT1. The selectivity ratio (Ki value for human SGLT2/Ki value for human SGLT1) of mizagliflozin is 303. Mizagliflozin shows the potential use for the amelioration of chronic constipation.

Targets

human SGLT1 ^[1]
(Cell-free assay)

27 nM(Ki)

In vitro

Mizagliflozin's inhibitory activity against SGLTs is evaluated by an in vitro assay of cells transiently expressing SGLTs. Mizagliflozin potently inhibits human SGLT1 in a highly selective manner.^[1].

In vivo

The oral administration of Mizagliflozin increased fecal wet weight in a dog model of loperamide-induced constipation and a rat model of low-fiber-diet-induced constipation.^[1].

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines COS-7 cells Concentrations 0-1 μM, 0-30 μM Incubation Time 1 h Method COS-7 cells are transiently transfected with a plasmid expressing human SGLT1 or SGLT2 by using Lipofectamine 2000. Two days after the transfection, the cells are incubated in an uptake buffer containing Mizagliflozin and 14C-labeled AMG at 37 ℃ for 1 h. The cells are then washed and their radioactivity is measured using Topcount. In this experiment, concentrations of 0.3 mM AMG and 1 mM AMG in the uptake buffer are used to calculate Ki values.
Animal Study:^{^[1]}	Animal Models Male Wistar rats, male Beagle dogs Dosages 2 mg/kg, 5 mg/kg, 10 mg/kg, 20 mg/kg, 40 mg/kg, 80 mg/kg, 160 mg/kg Administration Oral gavage

Cell Assay:^{^[1]}

Cell lines
COS-7 cells
Concentrations
0-1 μM, 0-30 μM
Incubation Time
1 h
Method
COS-7 cells are transiently transfected with a plasmid expressing human SGLT1 or SGLT2 by using Lipofectamine 2000. Two days after the transfection, the cells are incubated in an uptake buffer containing Mizagliflozin and 14C-labeled AMG at 37 ℃ for 1 h. The cells are then washed and their radioactivity is measured using Topcount. In this experiment, concentrations of 0.3 mM AMG and 1 mM AMG in the uptake buffer are used to calculate Ki values.

Animal Study:^{^[1]}

Animal Models
Male Wistar rats, male Beagle dogs
Dosages
2 mg/kg, 5 mg/kg, 10 mg/kg, 20 mg/kg, 40 mg/kg, 80 mg/kg, 160 mg/kg
Administration
Oral gavage

References

[1] Inoue T, et al. Eur J Pharmacol. 2017 Jul 5;806:25-31.

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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