Ipragliflozin (L-Proline) potently and selectively inhibits human, rat, and mouse SGLT2 at nanomolar concentrations and exhibits stability against intestinal glucosidases[3].
体内研究
Ipragliflozin (L-Proline) displays favorable pharmacokinetic properties and dose-dependently increases urinary glucose excretion, lasting for over 12 hours in normal mice[3].
Oral administration of Ipragliflozin increases urinary glucose excretion in a dose-dependent manner, with significant effects observed at doses of 0.3 mg/kg or higher, and this effect persists for over 12 hours[4].
Single administration of Ipragliflozin dose-dependently increases urinary glucose excretion, reduces blood glucose and plasma insulin levels, and improves glucose intolerance[1].
体外研究
Ipragliflozin (L-Proline) potently and selectively inhibits human, rat, and mouse SGLT2 at nanomolar concentrations and exhibits stability against intestinal glucosidases[3].
Ipragliflozin (L-Proline) 细胞实验
Cell Line
Concentration
Treated Time
Description
References
C2C12 cells
10 μM
Ipragliflozin enhanced C2C12 cell viability under hyperglycemic conditions, inhibited ferroptosis, and restored GPX4 expression.
Acta Pharmacol Sin. 2023 Jun;44(6):1161-1174.
Ipragliflozin (L-Proline) 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
Western diet-induced obese and diabetic mouse model
Oral administration via drinking water
10 mg/kg
Daily administration for 10 weeks
To evaluate the effect of Ipragliflozin on vascular remodeling. Results showed that Ipra increased adipocyte size in abdominal PVAT, reduced inflammation and fibrosis, and inhibited vascular remodeling.
Cardiovasc Diabetol. 2019 Jun 24;18(1):83
129S6/Sv mice
High-fat diet-induced obesity model
Oral gavage
10 mg/kg
Once daily for 16 weeks
To investigate the effect of ipragliflozin on energy metabolism in high-fat diet-induced obese mice. Results showed that ipragliflozin significantly attenuated HFD-induced hepatic steatosis, reduced adipocyte size, and upregulated thermogenesis-related gene expression in visceral and subcutaneous adipose tissue.
Diabetes Metab J. 2021 Nov;45(6):921-932
FLS-ob/ob mice
Non-alcoholic steatohepatitis (NASH) model
Oral gavage
1 mg/kg
Once daily for 12 weeks
Ipragliflozin improved lipid metabolism in FLS-ob/ob mice, reduced ectopic lipid deposition (ELD) in renal tubules, decreased endoplasmic reticulum stress (ER stress) and apoptosis, and attenuated interstitial fibrosis.
Int J Mol Sci. 2019 Dec 26;21(1):190
Mice
High-fat diet (HFD)-induced diabetic nephropathy model
Oral (via drinking water)
10 mg/kg
Once daily for 6 weeks
To investigate the effect of Ipra on HFD-induced diabetic nephropathy, results showed that Ipra reduced urinary albumin excretion (UAE) and glomerular hypertrophy, while increasing adipocyte size in PRAT and suppressing inflammation and fibrosis.
Int J Mol Sci. 2021 Jul 8;22(14):7329
C57BL/6JJcl mice
Streptozotocin (STZ)-induced diabetic mouse model
Oral
0.1 mg/kg or 3 mg/kg
Once daily for 4 weeks
To evaluate the protective effect of SGLT2 inhibitors on early pathogenic alterations in diabetic retinopathy. Results showed that ipragliflozin at a low dose (0.1 mg/kg/day) significantly suppressed retinal vascular leakage and retinal thickness without affecting blood glucose levels. Additionally, ipragliflozin attenuated microglial morphological changes and early pathogenic alterations.
Diabetes. 2024 Jul 1;73(7):1153-1166
Mice
DIO mice
Oral
0.002% in the diet
4 weeks
To evaluate the effects of ipragliflozin alone or in combination with liraglutide on glycemic control and hepatic lipid accumulation in DIO mice. Results showed that ipragliflozin improved glycemic control and reduced hepatic lipid accumulation.
Int J Mol Sci. 2021 Oct 25;22(21):11463
Mice
Db/db mice
Oral
0.001% in the diet
4 weeks
To evaluate the effects of ipragliflozin alone or in combination with liraglutide on glycemic control and hepatic lipid accumulation in db/db mice. Results showed that ipragliflozin improved glycemic control and reduced hepatic lipid accumulation.
Int J Mol Sci. 2021 Oct 25;22(21):11463
Mice
Type 2 diabetes model
Oral gavage
3 mg/kg/day and 0.3 mg/kg/day
Once daily for 8 weeks
To investigate the renoprotective effects of ipragliflozin on early diabetic nephropathy. High-dose ipragliflozin lowered blood glucose levels and reduced urinary albumin excretion, inhibited renal and glomerular hypertrophy, and reduced NADPH oxidase 4 expression and oxidative stress. A short-term ipragliflozin treatment improved oxygen tension in the kidney cortex.
Sci Rep. 2018 Mar 5;8(1):4029
Rats
Normal and type 2 diabetic Goto–Kakizaki (GK) rats
Ad libitum feeding
0.008% (w/w) mixed into diet
Daily for 20 days
To investigate the time-dependent effects of ipragliflozin on behaviour and energy homeostasis, results showed ipragliflozin increased food and water intakes, decreased blood glucose, and enhanced basal energy expenditure.
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