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].
体内研究
Administered orally in dosages ranging from 3 to 30 mg/kg, Mizagliflozin demonstrates a laxative effect[1].
When administered either intravenously at 0.3 mg/kg or orally at 3 mg/kg, Mizagliflozin is characterized by a short half-life, 0.23 hours and 1.14 hours respectively, indicating its rapid elimination from the body[2].
Mizagliflozin 细胞实验
Cell Line
Concentration
Treated Time
Description
References
mesangial cells (MCs)
10 and 100 nmol/L
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.
World J Diabetes. 2025 Jan 15;16(1):92711.
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.
Pharmacol Res Perspect. 2021 Oct;9(5):e00869.
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
Front Pharmacol. 2021 Jan 12;11:598353.
Mizagliflozin 动物实验
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.
World J Diabetes. 2025 Jan 15;16(1):92711.
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.
Pharmacol Res Perspect. 2021 Oct;9(5):e00869.
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
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