Home GPCR & G Protein SGLT inhibitor Mizagliflozin (KWA 0711)

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Mizagliflozin (KWA 0711) SGLT inhibitor

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 this compound is 303. It shows the potential use for the amelioration of chronic constipation.

Mizagliflozin (KWA 0711) SGLT inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 564.67

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

Related Products

Signaling Pathway

SGLT Signaling Pathways

SGLT Signaling Pathway

Mechanism of Action

Targets
human SGLT1 [1]
(Cell-free assay)
27 nM(Ki)

In vitro
In vitro

Mizagliflozin (KWA 0711) potently inhibits human SGLT1 in a highly selective manner, as evaluated by an in vitro assay of cells transiently expressing SGLTs.[1].
Cell Research Cell lines COS-7 cells
Concentrations 0-1 μM, 0-30 μM
Incubation Time 1 h
Method

In an experiment with Mizagliflozin (KWA 0711), 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 this compound and 14C-labeled AMG at 37 ℃ for 1 h. The cells are then washed and their radioactivity is measured using Topcount. Concentrations of 0.3 mM AMG and 1 mM AMG in the uptake buffer are used to calculate Ki values.

In Vivo
In vivo

In a dog model of loperamide-induced constipation and a rat model of low-fiber-diet-induced constipation, the oral administration of Mizagliflozin (KWA 0711) increased fecal wet weight.[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

References
  • https://pubmed.ncbi.nlm.nih.gov/28410751/

Chemical Information

Molecular Weight 564.67 Formula

C28H44N4O8
CAS No. 666843-10-3 SDF --
Synonyms N/A
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 and Stability

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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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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