Tofogliflozin(CSG 452)

For research use only.

Catalog No.S8558

Tofogliflozin(CSG 452) Chemical Structure

Molecular Weight(MW): 404.45

Tofogliflozin is a novel sodium-glucose co-transporter 2(SGLT2) inhibitor with IC50 values of 2.9 nM and 8444 nM for hSGLT2 and hSGLT1, respectively.

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Biological Activity

Description Tofogliflozin is a novel sodium-glucose co-transporter 2(SGLT2) inhibitor with IC50 values of 2.9 nM and 8444 nM for hSGLT2 and hSGLT1, respectively.
Targets
hSGLT2 [1]
(Cell-free assay)
2.9 nM
In vitro

Tofogliflozin is the potent and most selective inhibitor of SGLT2; the selectivity of tofogliflozin toward SGLT2 is 2900 times that toward SGLT1. Tofogliflozin dose-dependently inhibited glucose entry into tubular cells, tofogliflozin suppressed high glucose-induced ROS generation, MCP-1 gene induction and apoptosis in tubular cells and an antioxidant NAC mimicked the effects of tofogliflozin on high glucoseexposed tubular cells[3].

In vivo A single oral administration of this compound lowers blood glucose levels in Zucker diabetic rats with increased renal glucose clearance and treatment for 4 weeks with this compound improves glucose tolerance in db/db mice. Tofogliflozin treatment lowers urine volume compared with the untreated control group at 8 weeks of treatment. Tofogliflozin treatment increases renal glucose clearance levels compared with untreated db/db mice, whereas losartan treatment has no effect on this parameter. Tofogliflozin treatment reduces the threshold of glucose reabsorption in db/db mice and increases the UGE, and then reduces the PG. Tofogliflozin treatment significantly and dose-dependently elevates the total beta-cell mass, suggesting that beta-cell loss is prevented. Tofogliflozin suppresses plasma glucose and glycated Hb and preserves pancreatic beta-cell mass and plasma insulin levels[2].

Protocol

Cell Research:

[3]

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  • Cell lines: Tubular cells
  • Concentrations: 3 nM or 30 nM
  • Incubation Time: 24 h
  • Method:

    Tubular cells are treated with or without 3 nM or 30 nM tofogliflozin under serum-free BM containing 10 μg/ml transferrin and GA-1 000 for 24 h at 37 °C. Then, the cells are washed with PBS and incubated with Hanks’ balanced salt solution (HBSS) containing 100 μM of 2-[N-(7-nitrobenz-2-oxa-1,3-diazol-4-yl)amino]-2-deoxy-d-glucose (2-NBDG), a fluorescent derivative of glucose, in the absence of tofogliflozin for 15 min. Culture medium is removed and replaced with HBSS, and fluorescence intensity in the cells is analyzed in an ARVO fluorescent plate reader.


    (Only for Reference)
Animal Research:

[2]

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  • Animal Models: db/db mice
  • Dosages: 0.005 or 0.015%
  • Administration: oral
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 84 mg/mL (207.68 mM)
Ethanol 84 mg/mL (207.68 mM)
Water 4 mg/mL (9.88 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 404.45
Formula

C22H26O6.H2O

CAS No. 1201913-82-7
Storage powder
in solvent
Synonyms N/A
Smiles O.CCC1=CC=C(CC2=CC3=C(COC34OC(CO)C(O)C(O)C4O)C=C2)C=C1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID