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    Tofogliflozin
    Tofogliflozin

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V2750
    CAS #: ​903565-83-3 Purity ≥98%

    Description:  Tofogliflozin (also known as CSG-452) hydrate is a novel, very potent and highly selective inhibitor of sodium/glucose cotransporter 2 (SGLT2) with Ki values of 2.9, 14.9, and 6.4 nM for human, rat, and mouse respectively. Tofogliflozin competitively inhibited SGLT2 in cells that overexpress SGLT2. The selectivity of tofogliflozin towards human SGLT2 versus human SGLT1, SGLT6, and sodium/myo-inositol transporter 1 is the highest among the tested SGLT2 inhibitors under clinical trials. Long-term inhibition of renal SGLT2 by tofogliflozin not only preserved pancreatic beta-cell function, but also prevented kidney dysfunction in a mouse model of type 2 diabetes. These findings suggest that long-term use of tofogliflozin in patients with type 2 diabetes may prevent progression of diabetic nephropathy.

    References:  2012 Jun;341(3):692-701.

    Related CAS#:1201913-82-7 (hydrate) 


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    Molecular Weight (MW) 386.44
    Formula C22H26O6
    CAS No.903565-83-3 (free)  
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 10 mM
    Water: N/A
    Ethanol: N/A
    SMILES 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
    SynonymsCSG 452; CSG452; CSG-452; R-7201; R 7201; R7201


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    In Vitro

    In vitro activity: 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


    Kinase Assay: Tofogliflozin (also known as CSG-452) hydrate is a novel, very potent and highly selective inhibitor of sodium/glucose cotransporter 2 (SGLT2) with Ki values of 2.9, 14.9, and 6.4 nM for human, rat, and mouse respectively. Tofogliflozin competitively inhibited SGLT2 in cells that overexpress SGLT2. The selectivity of tofogliflozin towards human SGLT2 versus human SGLT1, SGLT6, and sodium/myo-inositol transporter 1 is the highest among the tested SGLT2 inhibitors under clinical trials. Long-term inhibition of renal SGLT2 by tofogliflozin not only preserved pancreatic beta-cell function, but also prevented kidney dysfunction in a mouse model of type 2 diabetes. These findings suggest that long-term use of tofogliflozin in patients with type 2 diabetes may prevent progression of diabetic nephropathy.


    Cell Assay: 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.

    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.
    Animal model db/db mice 
    Formulation & DosageCE2-pellets;  0.005 or 0.015%; oral 
    References  2013 Oct;170(3):519-31;  2016 Mar;48(3):191-5; J. Med. Chem., 2012, 55 (17), pp 7828–7840.


    These protocols are for reference only. InvivoChem does not independently validate these methods.


    Tofogliflozin

    Blood glucose and glycated Hb in db/db mice. 2013 Oct
     

    Tofogliflozin

    Urinary albumin excretion in db/db and db/ + m mice.  2013 Oct
     

    Tofogliflozin

    Histological analyses of glomeruli at 8 weeks of treatment (2).  2013 Oct


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