Tofogliflozin (hydrate)_product_DataBase

Bioactivity

Tofogliflozin hydrate (CSG-452 hydrate) is a potent and highly specific sodium/glucose cotransporter 2 (SGLT2) inhibitor with an IC50 of 2.9 nM and Ki values of 2.9 nM, 14.9 nM, and 6.4 nM for human, rat, and mouse SGLT2[1]. Tofogliflozin partially inhibits high glucose-induced reactive oxyen species (ROS) generation in tubular cells[2].

Target

IC50: 2.9 nM (SGLT2); Ki: 2.9 nM ( human SGLT2), 14.9 nM (rat SGLT2), and 6.4 nM (mouse SGLT2)

Invitro

Tofofloxacin (3-30 nM; 24 hours; tubular epithelial cells) treatment inhibits the oxidative stress generation and monocyte chemoattractant protein-1 (MCP-1) gene expression in tubular cells induced by high glucose[2].Tofofloxacin (3-30 nM; 8 days; tubular epithelial cells) treatment inhibits the apoptotic cell death induced by high glucose[2]. RT-PCR[2] Cell Line:

In Vivo

Tofogliflozin (0.1-10 mg/kg; oral administration; once daily; for 4 weeks; db/db mice) treatment improves hyperglycemia and thereby ameliorated glucose intolerance of the obese diabetic mice[1]. Animal Model:

Name

Tofogliflozin (hydrate)

CAS

1201913-82-7

Formula

C22H28O7

Molar Mass

404.45

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[1]. Suzuki M, et al. Tofogliflozin, a potent and highly specific sodium/glucose cotransporter 2 inhibitor, improves glycemic control in diabetic rats and mice. J Pharmacol Exp Ther. 2012 Jun;341(3):692-701. [2]. Ishibashi Y, et al. Tofogliflozin, A Highly Selective Inhibitor of SGLT2 Blocks Proinflammatory and Proapoptotic Effects of Glucose Overload on Proximal Tubular Cells Partly by Suppressing Oxidative Stress Generation. Horm Metab Res. 2016 Mar;48(3):191-5.

PeptideDB

Tofogliflozin (hydrate)

CAS: 1201913-82-7 F: C22H28O7 W: 404.45