Mizagliflozin (KWA 0711)

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.

Mizagliflozin (KWA 0711) Chemical Structure

Mizagliflozin (KWA 0711) Chemical Structure

CAS: 666843-10-3

Purity & Quality Control

Batch: S893901 DMSO] 100 mg/mL] false] Water] 100 mg/mL] false] Ethanol] 100 mg/mL] false Purity: 99.59%
99.59

Mizagliflozin (KWA 0711) Related Products

Signaling Pathway

Choose Selective SGLT Inhibitors

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
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].

Cell Research 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.

In Vivo
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].

Animal Research 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
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05541939 Completed
Postbariatric Hypoglycemia
Vogenx Inc.
September 13 2022 Phase 2

Chemical Information & Solubility

Molecular Weight 564.67 Formula

C28H44N4O8

CAS No. 666843-10-3 SDF --
Smiles CC1=C(C=CC(=C1)OCCCNCC(C)(C)C(=O)N)CC2=C(NN=C2OC3C(C(C(C(O3)CO)O)O)O)C(C)C
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (177.09 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 100 mg/mL

Ethanol : 100 mg/mL


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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