Ipragliflozin-13C6 is intended for use as an internal standard for the quantification of ipragliflozin by GC- or LC-MS. Ipragliflozin is a sodium-glucose cotransporter 2 (SGLT2) inhibitor (IC50 = 7.4 nM in CHO cells expressing the human cotransporter).1 It is selective for SGLT2 over SGLT1, SGLT3, SGLT4, SGLT5, and SGLT6 (IC50s = 1.9, 30.4, 15.9, 0.46, and 10.4 µM, respectively). Ipragliflozin (0.1-3 mg/kg) decreases plasma levels of insulin and glucose in an oral glucose tolerance test in a mouse model of diabetes induced by high-fat diet, streptozotocin , and nicotinamide .2 It decreases plasma and hepatic IL-6, TNF-α, chemokine (C-C motif) ligand 2 (CCL2), and C-reactive protein (CRP) levels in the same model when administered at a dose of 3 mg/kg per day for 28 days.
1.Takasu, T., Yokono, M., Tahara, A., et al.In vitro pharmacological profile of ipragliflozin, a sodium glucose co-transporter 2 inhibitorBiol. Pharm. Bull.42(3)507-511(2019) 2.Tahara, A., Kurosaki, E., Yokono, M., et al.Effects of SGLT2 selective inhibitor ipragliflozin on hyperglycemia, hyperlipidemia, hepatic steatosis, oxidative stress, inflammation, and obesity in type 2 diabetic miceEur. J. Pharmacol.715(1-3)246-255(2013)