1. Membrane Transporter/Ion Channel
    Metabolic Enzyme/Protease
    Immunology/Inflammation
    NF-κB
  2. SGLT
    Reactive Oxygen Species
  3. Tofogliflozin (hydrate)

Tofogliflozin (hydrate) (Synonyms: CSG-452 hydrate)

Cat. No.: HY-13413 Purity: 99.41%
Handling Instructions

Tofogliflozin hydrate (CSG-452 hydrate) is a potent and highly specific sodium/glucose cotransporter 2 (SGLT2) inhibitor with an IC50 of 2.9 nM and Ki values of 2.9 nM, 14.9 nM, and 6.4 nM for human, rat, and mouse SGLT2. Tofogliflozin partially inhibits high glucose-induced reactive oxyen species (ROS) generation in tubular cells.

For research use only. We do not sell to patients.

Tofogliflozin (hydrate) Chemical Structure

Tofogliflozin (hydrate) Chemical Structure

CAS No. : 1201913-82-7

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Based on 2 publication(s) in Google Scholar

Other Forms of Tofogliflozin (hydrate):

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Description

Tofogliflozin hydrate (CSG-452 hydrate) is a potent and highly specific sodium/glucose cotransporter 2 (SGLT2) inhibitor with an IC50 of 2.9 nM and Ki values of 2.9 nM, 14.9 nM, and 6.4 nM for human, rat, and mouse SGLT2[1]. Tofogliflozin partially inhibits high glucose-induced reactive oxyen species (ROS) generation in tubular cells[2].

IC50 & Target

IC50: 2.9 nM (SGLT2); Ki: 2.9 nM ( human SGLT2), 14.9 nM (rat SGLT2), and 6.4 nM (mouse SGLT2)[1]

In Vitro

Tofofloxacin (3-30 nM; 24 hours; tubular epithelial cells) treatment inhibits the oxidative stress generation and monocyte chemoattractant protein-1 (MCP-1) gene expression in tubular cells induced by high glucose[2].
Tofofloxacin (3-30 nM; 8 days; tubular epithelial cells) treatment inhibits the apoptotic cell death induced by high glucose[2].

RT-PCR[2]

Cell Line: Tubular epithelial cells
Concentration: 3 nM and 30 nM
Incubation Time: 24 hours
Result: Inhibited MCP-1 gene expression in tubular cells induced by high glucose exposure.

Apoptosis Analysis[2]

Cell Line: Tubular epithelial cells
Concentration: 3 nM and 30 nM
Incubation Time: 8 days
Result: Inhibited the apoptotic cell death induced by high glucose.
In Vivo

Tofogliflozin (0.1-10 mg/kg; oral administration; once daily; for 4 weeks; db/db mice) treatment improves hyperglycemia and thereby ameliorated glucose intolerance of the obese diabetic mice[1].

Animal Model: db/db mice[1]
Dosage: 0.1 mg/kg, 0.3 mg/kg, 1 mg/kg, 3 mg/kg, or 10 mg/kg
Administration: Oral administration; once daily; for 4 weeks
Result: Observed acute blood glucose reduction, dose-dependently reduced glycated hemoglobin, significantly prevented the decrease of IRI levels at doses of 3 and 10 mg/kg, and no difference in food intake or body weight.
Clinical Trial
Molecular Weight

404.45

Formula

C₂₂H₂₈O₇

CAS No.

1201913-82-7

SMILES

O[[email protected]@H]1[[email protected]@H](O)[[email protected]](O)[[email protected]@H](CO)O[[email protected]@]21OCC3=C2C=C(CC4=CC=C(CC)C=C4)C=C3.O

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (247.25 mM)

H2O : 0.33 mg/mL (0.82 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4725 mL 12.3625 mL 24.7249 mL
5 mM 0.4945 mL 2.4725 mL 4.9450 mL
10 mM 0.2472 mL 1.2362 mL 2.4725 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.18 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.18 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.18 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.41%

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Tofogliflozin (hydrate)
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