[CAS NO. 1201913-82-7] Tofogliflozin(CSG 452)

Name: Tofogliflozin(CSG 452)
Brand: Arctom Scientific
SKU: SLK-S8558

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PRODUCTS SPECIFICATIONS [1201913-82-7]

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Catalog

SLK-S8558

Brand

Selleck

CAS

1201913-82-7

DESCRIPTION [1201913-82-7]

Overview

MDL	-
Molecular Weight	404.45
Molecular Formula	C22H26O6.H2O
SMILES	O[C@H]1[C@]2(C=3C(CO2)=CC=C(CC4=CC=C(CC)C=C4)C3)O[C@H](CO)[C@@H](O)[C@@H]1O.O

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.4725 mL	12.3625 mL	24.7249 mL
5 mM	0.4945 mL	2.4725 mL	4.9450 mL
10 mM	0.2472 mL	1.2362 mL	2.4725 mL
50 mM	0.0494 mL	0.2472 mL	0.4945 mL

Description

Tofogliflozin (CSG 452) is a novel 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.

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.

References

[1] Yoshihito Ohtake, et al. J Med Chem. 2012, 55(17):7828-7840.
[2] Nagata T, et al. Br J Pharmacol. 2013, 170(3):519-31.
[3] Ishibashi Y, et al. Horm Metab Res. 2016, 48(3):191-5.

Synonyms

Spiro[isobenzofuran-1(3H),2′-[2H]pyran]-3′,4′,5′-triol, 6-[(4-ethylphenyl)methyl]-3′,4′,5′,6′-tetrahydro-6′-(hydroxymethyl)-, hydrate (1:1), (1S,3′R,4′S,5′S,6′R)-

Deberza

Tofogliflozin hydrate