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.
| 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 |
| 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.
| Related SGLT Products |
|---|
| Tianagliflozin
Tianagliflozin is an SGLT2 inhibitor that may be used in studies related to type 2 diabetes. |
| JTT-662
JTT-662 is an SGLT1 inhibitor that can be used in studies related to type 2 diabetes. |
| JP-2266
JP-2266 is a dual SGLT1/2 inhibitor that can be used in studies related to diabetes. |
| Tofogliflozin
Tofogliflozin(CSG-452) is a potent and highly specific sodium/glucose cotransporter 2(SGLT2) inhibitor with Ki values of 2.9, 14.9, and 6.4 nM for human, rat, and mouse SGLT2. |
| Mizagliflozin
Mizagliflozin (DSP-3235 free base) is a potent, orally active and selective SGLT1 inhibitor, with a Ki of 27 nM for human SGLT1. Mizagliflozin displays 303-fold selectivity over SGLT2. Mizagliflozin is used as an antidiabetic agent that can modify postprandial blood glucose excursion. Mizagliflozin also exhibits potential in the amelioration of chronic constipation. |
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