Tofogliflozin is a potent and highly specific sodium/glucose cotransporter 2(SGLT2) inhibitor with Ki values of 2.9, 14.9, and 6.4 nM for human, rat, and mouse SGLT2.
Tofogliflozin (hydrate)/托格列净一水合物 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
Db/db mice (type 2 diabetes model)
Oral (dietary addition)
0.005% or 0.015% (w/w)
Continuous for 8 weeks
To evaluate the long-term effects of tofogliflozin on renal and pancreatic function in db/db mice. Results showed that tofogliflozin significantly reduced plasma glucose and glycated Hb levels, preserved pancreatic beta-cell mass and plasma insulin levels, and prevented the progression of kidney dysfunction.
Br J Pharmacol. 2013 Oct;170(3):519-31
Rats and mice
Diet-induced obese (DIO) rats and KKAy mice
Oral
0.05% tofogliflozin (HFD/TOFO), 0.015 or 0.0015% tofogliflozin (CE-2/TOFO)
9 weeks in DIO rats, 3 or 5 weeks in KKAy mice
Tofogli?ozin attenuates body weight gain mainly due to calorie loss with increased UGE. In addition, tofogli?ozin also induces a metabolic shift from carbohydrate oxidation to fatty acid oxidation, which may lead to prevention of fat accumulation and in?ammation in adipose tissue and liver.
Nutr Diabetes. 2014 Jul 7;4(7):e125
Male F344/NSlc rats
CCl4-induced cirrhotic and portal hypertension model
Oral gavage
10 or 20 mg/kg
Daily administration for 14 weeks
To evaluate the effect of tofogliflozin on portal hypertension and hepatic fibrosis. Results showed that tofogliflozin prevented the development of portal hypertension, attenuated intrahepatic vasoconstriction, sinusoidal capillarization, and remodeling, and suppressed hepatic macrophage infiltration, proinflammatory response, and fibrogenesis, independent of glycemic status.
Cells. 2024 Mar 19;13(6):538
Human
Type 2 diabetes patients
Oral
10, 20, 40 mg
24 weeks
To examine the effects of tofogliflozin on resting heart rate, results showed that tofogliflozin significantly reduced resting heart rate, which was correlated with baseline levels.
Diabet Med. 2020 Aug;37(8):1316-1325
Sprague-Dawley rats
Renal congestion model
Oral
3.0 mg/kg/day
Once daily, from the day before surgery until two days after surgery
Tofogliflozin improved the increased kidney weight and water content caused by renal congestion, reduced renal injury and fibrosis, particularly in the renal cortex. Additionally, Tofogliflozin reduced the expression of inflammatory molecules and improved mitochondrial dysfunction.
Hypertens Res. 2024 Jan;47(1):33-45
Mice
Type 2 diabetic mouse model
Oral
5 mg/kg/day
Once daily for 8 weeks
To investigate the effect of Tofogliflozin on retinal blood flow dysregulation, neural retinal dysfunction, and impaired neurovascular coupling in type 2 diabetic mice. Results showed that Tofogliflozin treatment significantly improved retinal neurovascular coupling function and inhibited retinal glial activation in diabetic mice.
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