Mizagliflozin

For research use only.

Catalog No.S8939 Synonyms: KWA 0711

Mizagliflozin Chemical Structure

Molecular Weight(MW): 564.67

Mizagliflozin 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.

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Biological Activity

Description Mizagliflozin 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

Cell Research:

[1]

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  • 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.


    (Only for Reference)
Animal Research:

[1]

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  • 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
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (177.09 mM)
Water 100 mg/mL (177.09 mM)
Ethanol '100 mg/mL

* 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.

Chemical Information

Molecular Weight 564.67
Formula

C28H44N4O8

CAS No. 666843-10-3
Storage powder
in solvent
Synonyms KWA 0711

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SGLT Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID