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Tofogliflozin (hydrate)

Cat. No. M10441
Tofogliflozin (hydrate) Structure

CSG-452 hydrate

Size Price Availability Quantity
5mg USD 90  USD100 In stock
10mg USD 126  USD140 In stock
50mg USD 432  USD480 In stock
100mg USD 594  USD660 In stock
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Quality Control
  • Current batch:
  • Purity >98.5%
  • COA
  • MSDS
Biological Activity

Tofogliflozin (CSG-452) hydrate is a potent and highly specific sodium-glucose co-transporter 2(SGLT2) inhibitor with IC50 value of 2.9 nM. 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, Tofogliflozin (0.1-10 mg/kg; oral administration; once daily for 4 weeks) treatment improves hyperglycemia and thereby ameliorated glucose intolerance of the obese diabetic mice.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 404.45
Formula C22H26O6.H2O
CAS Number 1201913-82-7
Purity >98.5%
Solubility DMSO 80 mg/mL
Water ~1 mg/mL
Storage at -20°C

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
Y Ishibashi, et al. Horm Metab Res. 2016 Mar;48(3):191-5. PMID: 26158396.

Tofogliflozin, a potent and highly specific sodium/glucose cotransporter 2 inhibitor, improves glycemic control in diabetic rats and mice
Masayuki Suzuki, et al. J Pharmacol Exp Ther. 2012 Jun;341(3):692-701. PMID: 22410641.

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LX-4211 is an oral dual SGLT1/SGLT2 inhibitor with IC50 of 36 nM and 1.8 nM, respectively.

Abmole Inhibitor Catalog 2017

Keywords: Tofogliflozin (hydrate), CSG-452 hydrate supplier, SGLT, inhibitors

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