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Tofogliflozin (hydrate)

Cat. No. M10441
Tofogliflozin (hydrate) Structure
Synonym:

CSG-452 hydrate

Size Price Availability Quantity
5mg USD 100  USD100 In stock
10mg USD 140  USD140 In stock
50mg USD 480  USD480 In stock
100mg USD 660  USD660 In stock
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Quality Control & Documentation
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.

Chemical Information
Molecular Weight 404.45
Formula C22H26O6.H2O
CAS Number 1201913-82-7
Solubility (25°C) DMSO 80 mg/mL
Water ~1 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Y Ishibashi, et al. Horm Metab Res. 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

[2] Masayuki Suzuki, et al. J Pharmacol Exp Ther. Tofogliflozin, a potent and highly specific sodium/glucose cotransporter 2 inhibitor, improves glycemic control in diabetic rats and mice

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

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