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Chemical Structure| 666843-10-3 Chemical Structure| 666843-10-3

Structure of Mizagliflozin
CAS No.: 666843-10-3

Chemical Structure| 666843-10-3

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Mizagliflozin is an effective SGLT1 inhibitor that improves postprandial blood glucose levels by inhibiting sodium-glucose co-transporter in the small intestine and aids in the treatment of chronic constipation. It holds application prospects in diabetes and gastrointestinal disease research.

Synonyms: DSP-3235 free base; KGA-3235 free base; GSK-1614235

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Product Details of Mizagliflozin

CAS No. :666843-10-3
Formula : C28H44N4O8
M.W : 564.67
SMILES Code : CC1=C(C=CC(OCCCNCC(C)(C(N)=O)C)=C1)CC2=C(C(C)C)NN=C2O[C@H]3[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O3
Synonyms :
DSP-3235 free base; KGA-3235 free base; GSK-1614235
MDL No. :MFCD30533437

Safety of Mizagliflozin

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Isoform Comparison

Biological Activity

Description
Mizagliflozin (DSP-3235 free base) is a potent, orally active inhibitor specifically targeting the SGLT1 transporter, with a Ki of 27 nM for human SGLT1, showcasing a 303-fold selectivity over SGLT2. This selectivity positions Mizagliflozin as a promising antidiabetic agent capable of modifying postprandial blood glucose levels. Additionally, it has shown potential in alleviating symptoms of chronic constipation[1].

In Vitro:

Cell Line
Concentration Treated Time Description References
mesangial cells (MCs) 10 and 100 nM 3 days To evaluate the effect of MIZ on glucose consumption in mesangial cells under high glucose conditions. Results showed that MIZ significantly reduced glucose consumption under high glucose conditions in a dose-dependent manner. PMC11718448
PC12HS cells 1 μM or 10 μM 48 h To investigate the effects of Mizagliflozin on SGLT1 and MCP-1 gene expressions in IL-1β-stimulated PC12HS cells. Results showed that IL-1β increased mRNA expressions of SGLT1 and MCP-1, and mizagliflozin did not reduce their increased gene expressions but improved IL-1β-induced cell death. PMC8480397
H9C2 cardiomyocytes 10, 20, or 40 µM 24 h To investigate the effect of Mizagliflozin on high glucose-induced apoptosis in H9C2 cells, results showed that Mizagliflozin significantly reduced the expression of apoptosis-related proteins and mRNA and the proportion of TUNEL-positive cells PMC7883645

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Db/db mice Diabetic nephropathy model Oral gavage 0.5 mg/kg and 1.0 mg/kg Once daily for 8 weeks To evaluate the effect of MIZ on renal damage in diabetic nephropathy mice. Results showed that high-dose MIZ significantly reduced blood glucose levels and food intake, while alleviating renal damage and inflammatory responses. PMC11718448
C57BL/6J male mice Asymmetric common carotid artery stenosis surgery (ACAS) model Subcutaneous injection 100 μg/μl or 500 μg/μl 42 days or 30 days To investigate the effects of Mizagliflozin on vascular cognitive impairment in ACAS mice. Results showed that Mizagliflozin improved cognitive impairment and neuronal death in ACAS mice but did not improve the decreased cerebral blood flow or the increased inflammatory gene expressions. PMC8480397
Wistar rats Diabetic cardiomyopathy model Gavage 0.5, 1.0, or 1.5 mg/kg Once daily for 12 weeks To investigate the effect of Mizagliflozin on cardiac function and myocardial fibrosis in diabetic cardiomyopathy rats, results showed that Mizagliflozin significantly improved cardiac function and alleviated myocardial fibrosis and apoptosis PMC7883645

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT05541939 Postbariatric Hypoglycemia PHASE2 COMPLETED 2023-02-17 Stanford, Palo Alto, Californi... More >>a, 94304, United States|University of Colorado / Anschutz Medical Campus, Aurora, Colorado, 80045, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.77mL

0.35mL

0.18mL

8.85mL

1.77mL

0.89mL

17.71mL

3.54mL

1.77mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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