Ipragliflozin (ASP1941) is an orally active and selective SGLT2 inhibitor with IC50s of 7.38 and 1876 nM, 6.73 and 1166 nM, 5.64 and 1380 nM for human SGLT2 and SGLT1, rat SGLT2 and SGLT1, mouse SGLT2 and SGLT1, respectively. SGLT2 selective inhibitor ipragliflozin exerts a beneficial effect on glycaemic control and ameliorates diabetes-associated metabolic abnormalities and complications in STZ-induced diabetic rats, and would be a potential agent for the treatment of type 1 diabetes.
Cell Experiment | |
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Cell lines | MCF-7 human breast cancer cell lines |
Preparation method | Cell proliferation assays Briefly, cells were seeded in 12-well tissue culture plates and maintained in complete medium with 0-50 μM ipragliflozin. Cell proliferation was analyzed 0-4 days later by cell counting using a hemocytometer. |
Concentrations | 1, 10, 50 μM |
Incubation time | 24, 48, 72, 96 hours |
Animal Experiment | |
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Animal models | Male C57BL/6J wild-type (WT) mice, Male C57BL/6J-ob/ob (ob/ob) mice |
Formulation | DMSO |
Dosages | 10 mg/kg/day |
Administration | Oral gavage |
Molecular Weight | 404.45 |
Formula | C21H21FO5S |
CAS Number | 761423-87-4 |
Solubility (25°C) | DMSO ≥ 60 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.
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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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