Home GPCR & G Protein SGLT inhibitor Tofogliflozin(CSG 452) For research use only.

Tofogliflozin(CSG 452)

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.

Tofogliflozin(CSG 452) Chemical Structure

Tofogliflozin(CSG 452) Chemical Structure

CAS No. 1201913-82-7

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Tofogliflozin(CSG 452) Related Products

Signaling Pathway

SGLT Signaling Pathways

SGLT Signaling Pathway

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
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].
Cell Research 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.
In Vivo
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].
Animal Research Animal Models db/db mice
Dosages 0.005 or 0.015%
Administration oral
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05722262 Completed
Healthy
Kowa Research Institute Inc.
 February 24 2023 Phase 1

Chemical Information & Solubility

Molecular Weight 404.45 Formula

C22H26O6.H2O
CAS No. 1201913-82-7 SDF Download Tofogliflozin(CSG 452) SDF
Smiles CCC1=CC=C(C=C1)CC2=CC3=C(COC34C(C(C(C(O4)CO)O)O)O)C=C2.O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 84 mg/mL ( (207.68 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 84 mg/mL

Water : 4 mg/mL


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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