Dapagliflozin-d5

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 (K_i = 6 nM; EC₅₀ = 1.1 nM) over SGLT1 (K_i = 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)