Tofogliflozin(CSG 452)

Catalog No.S8558 Batch:S855801

Technical Data

Formula	C₂₂H₂₆O₆.H₂O
Molecular Weight	404.45	CAS No.	1201913-82-7
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)
* <1 mg/ml means slightly soluble or insoluble. * 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

Tofogliflozin (CSG 452) 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 (from reference)

Cell Assay:^{^[3]}	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.
Animal Study:^{^[2]}	Animal Models db/db mice Dosages 0.005 or 0.015% Administration oral

Cell Assay:^{^[3]}

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.

Animal Study:^{^[2]}

Animal Models
db/db mice
Dosages
0.005 or 0.015%
Administration
oral

References

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SHIPPING AND STORAGE
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