Tofogliflozin hydrate

SKU: orb1226811

Description

Tofogliflozin (CSG-452) is a potent, highly selective SGLT2 inhibitor with Ki of 2.9, 14.9, and 6.4 nM against human, rat, and mouse SGLT2, respectively; displays high selectivity over human SGLT2 versus human SGLT1, SGLT6, and sodium/myo-inositol transporter 1; increases renal glucose clearance and lowered the blood glucose level in Zucker diabetic fatty rats, also improves postprandial glucose excursion; reduces glycated hemoglobin and improved glucose tolerance in the oral glucose tolerance test in vivo.Diabetes Approved(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.Tofofloxacin (3-30 nM; 8 days; tubular epithelial cells) treatment inhibits 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.

Key Properties

• CAS Number: 1201913-82-7
• MW: 404.5
• Purity: >98% (HPLC)
• Formula: C₂₂H₂₈O₇
• SMILES: CCC1=CC=C(C=C1)CC2=CC3=C(COC34C(C(C(C(O4)CO)O)O)O)C=C2.O
• Target: SGLT
• Solubility: 10 mM in DMSO

Bioactivity

• 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. Animal model: db/db mice. 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.
• 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. Tofofloxacin (3-30 nM; 8 days; tubular epithelial cells) treatment inhibits the apoptotic cell death induced by high glucose. RT-PCR 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 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CSG452 hydrate | CSG-452 hydrate

Quick Database Links

Gene Symbol

SGLT