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Ipragliflozin

Cat. No. M5254
Ipragliflozin Structure
Synonym:

ASP 1941

Size Price Availability Quantity
5mg USD 50  USD50 In stock
10mg USD 70  USD70 In stock
25mg USD 100  USD100 In stock
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Quality Control & Documentation
Biological Activity

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.

Protocol (for reference only)
Cell Experiment
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
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
Chemical Information
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
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] Komiya C, et al. PLoS One. Ipragliflozin Improves Hepatic Steatosis in Obese Mice and Liver Dysfunction in Type 2 Diabetic Patients Irrespective of Body Weight Reduction.

[2] Kashiwagi A, et al. Diabetes Obes Metab. Ipragliflozin in combination with metformin for the treatment of Japanese patients with type 2 diabetes: ILLUMINATE, a randomized, double-blind, placebo-controlled study.

[3] Tahara A, et al. J Pharm Pharmacol. Effects of sodium-glucose cotransporter 2 selective inhibitor ipragliflozin on hyperglycaemia, oxidative stress, inflammation and liver injury in streptozotocin-induced type 1 diabetic rats.

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Keywords: Ipragliflozin, ASP 1941 supplier, SGLT, inhibitors, activators


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