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Chemical Structure| 1201913-82-7 Chemical Structure| 1201913-82-7

Structure of Tofogliflozin (hydrate)
CAS No.: 1201913-82-7

Chemical Structure| 1201913-82-7

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Tofogliflozin hydrate (CSG-452 hydrate) is a potent, highly specific, and selective SGLT2 inhibitor with an IC50 of 2.9 nM for human, 14.9 nM for rat, and 6.4 nM for mouse SGLT2. Tofogliflozin hydrate partially inhibits high glucose-induced ROS production in renal tubular cells.

Synonyms: CSG-452 hydrate; CSG 452; Tofogliflozin

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Product Details of Tofogliflozin (hydrate)

CAS No. :1201913-82-7
Formula : C22H28O7
M.W : 404.45
SMILES Code : O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@]21OCC3=C2C=C(CC4=CC=C(CC)C=C4)C=C3.[H]O[H]
Synonyms :
CSG-452 hydrate; CSG 452; Tofogliflozin
MDL No. :MFCD28385880

Safety of Tofogliflozin (hydrate)

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

Target
  • SGLT2

    hSGLT2, IC50:2.9 nM

In Vivo:

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. Int J Mol Sci. 2022 Jan 25;23(3):1362

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.47mL

0.49mL

0.25mL

12.36mL

2.47mL

1.24mL

24.72mL

4.94mL

2.47mL

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
The prepared working fluid is recommended to be prepared now and used up as soon as possible in a short period of time. 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

References

 

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