Tofogliflozin(CSG 452)

Catalog No.S8558 Batch:S855802

Technical Data

Formula

C₂₂H₂₆O₆.H₂O

Molecular Weight

404.45

CAS No.

1201913-82-7

Solubility (25°C)*

In vitro

DMSO

80 mg/mL (197.79 mM)

Ethanol

80 mg/mL (197.79 mM)

Water

3 mg/mL (7.41 mM)

In vivo (Add solvents to the product individually and in order)

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <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 (CSG 452) is a potent and highly selective SGLT2 inhibitor, with 2900-fold greater selectivity for SGLT2 over SGLT1. It dose-dependently inhibited glucose entry into tubular cells, suppressed high glucose-induced ROS generation, MCP-1 gene induction, and apoptosis in tubular cells. An antioxidant NAC mimicked the effects of this compound on high glucose-exposed tubular cells^[3].

In vivo

Tofogliflozin (CSG 452), when administered as a single oral dose, lowers blood glucose levels in Zucker diabetic rats by increasing renal glucose clearance. A four-week treatment with this compound improves glucose tolerance in db/db mice. It also reduces urine volume compared with the untreated control group at 8 weeks of treatment. Compared with untreated db/db mice, treatment increases renal glucose clearance levels, whereas losartan has no effect on this parameter. It reduces the threshold of glucose reabsorption in db/db mice, increases UGE, and subsequently lowers PG. Additionally, treatment significantly and dose-dependently elevates total beta-cell mass, suggesting prevention of beta-cell loss. Tofogliflozin suppresses plasma glucose and glycated Hb while preserving 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 (CSG 452) under serum-free BM containing 10 μg/ml transferrin and GA-1 000 for 24 h at 37 °C. After washing with PBS, the cells are 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 this compound 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 (CSG 452) under serum-free BM containing 10 μg/ml transferrin and GA-1 000 for 24 h at 37 °C. After washing with PBS, the cells are 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 this compound 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

http://pubs.acs.org/doi/abs/10.1021/jm300884k
https://pubmed.ncbi.nlm.nih.gov/23751087/
https://pubmed.ncbi.nlm.nih.gov/26158396/

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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