Dapagliflozin-d5 is intended for use as an internal standard for the quantification of dapagliflozin by GC- or LC-MS. Dapagliflozin is a first generation, selective sodium-glucose linked transporter (SGLT) inhibitor that blocks glucose transport with about 100-fold selectivity for SGLT2 (Ki = 6 nM; EC50 = 1.1 nM) over SGLT1 (Ki = 390 nM).1 After single oral doses ranging from 0.1 to 1.0 mg/kg, dapagliflozin increases urinary glucose excretion in both normal and diabetic rats, improves glucose tolerance in normal rats, and reduces hyperglycemia in Zucker diabetic fatty rats.2 Within two weeks of treating diabetic rats with 0.1 to 1.0 mg/kg dapagliflozin, fasting and fed glucose levels have been shown to be significantly lowered as a result of increased glucose utilization accompanied by reduced glucose production.
1.Chao, E.C., and Henry, R.R.SGLT2 inhibition - A novel strategy for diabetes treatmentNature Reviews.Drug Discovery9(7)551-559(2010) 2.Han, S., Hagan, D.L., Taylor, J.R., et al.Dapagliflozin, a selective SGLT2 inhibitor, improves glucose homeostasis in normal and diabetic ratsDiabetes57(6)1723-1729(2008)