Description
Dapagliflozin is a potent and selective inhibitor of hSGLT2 with EC50 of 1.1 nM, exhibiting 1200-fold selectivity over hSGLT1.
Product Overview
Selective inhibition of SGLT2 has been proposed to aid in the normalization of plasma glucose levels in patients with diabetes by preventing the renal glucose reabsorption process and promoting glucose excretion in urine. Dapagliflozin is a potent, selective Renal Sodium-Dependent Glucose Cotransporter 2 (SGLT2) inhibitor.
Molecular Formula
C21H25ClO6
Chemical Name
(2S,3R,4R,5S,6R)-2-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-6-(hydroxymethyl)oxane-3,4,5-triol
Solubility
Soluble in DMSO > 10 mM
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
In vitro
EC50 values of 1.1 nM for hSGLT2 and 1.4 μM for hSGLT1 determined for Dapagliflozin corresponded to 1200-fold selectivity for SGLT2 as compared with phlorizin's 10-fold selectivity. Dapagliflozin inhibitory potencies against rat SGLT (rSGLT)2 and hSGLT2 were comparable, but the selectivity of Dapagliflozin for rSGLT2 versus rSGLT1 decreased to 200-fold.
In vivo
In vivo, dapagliflozin acutely induced renal glucose excretion in diabetic and normal rats, improved glucose tolerance in normal rats, as well as reduced hyperglycemia in Zucker diabetic fatty rats after single oral doses ranging between 0.1 and 1.0 mg/kg levels and body weight in treatment-naive patients with type 2 diabetes. Dapagliflozin was well tolerated.
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