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Tofogliflozin(CSG 452) SGLT inhibitor

Name: Tofogliflozin(CSG 452)
SKU: S8558
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S8558

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.

Chemical Structure

Molecular Weight: 404.45

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.92%

99.92

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Chemical Information, Storage & Stability

Molecular Weight	404.45	Formula	C₂₂H₂₆O₆.H₂O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1201913-82-7	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CCC1=CC=C(C=C1)CC2=CC3=C(COC34C(C(C(C(O4)CO)O)O)O)C=C2.O

Solubility

In vitro
Batch:

DMSO : 84 mg/mL (207.68 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 84 mg/mL

Water : 4 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
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.
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.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	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].
References	[1] http://pubs.acs.org/doi/abs/10.1021/jm300884k [2] https://pubmed.ncbi.nlm.nih.gov/23751087/ [3] https://pubmed.ncbi.nlm.nih.gov/26158396/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05722262	Completed	Healthy	Kowa Research Institute Inc.	February 24 2023	Phase 1

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