Dapagliflozin 461432-26-8

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Molecular Weight:

408.87 Dapagliflozin is a potent and selective hSGLT2 inhibitor with EC50 of 1.1 nM, exhibiting 1200-fold selectivity over hSGLT1. Phase 4.

Biological Activity

Dapagliflozin is not sensitive to hSGLT1 with a 1200-fold IC50. Dapagliflozin is 32-fold more potent than phlorizin against hSGLT2 but
4-fold less than phlorizin against hSGLT1. Dapagliflozin is highly
selective versus GLUT transporters and displays 8–9% inhibition in
protein-free buffer at 20 μM and virtually no inhibition in the presence
of 4% bovine serum albumin.


Dapagliflozin has good
permeability across Caco-2 cell membranes and is a substrate for
P-glycoprotein (P-gp) but not a significant P-gp Inhibitor.
Dapagliflozin is stable in rat, dog, monkey, and human serum at 10 μM.
Dapagliflozin shows no inhibitory responses or induction to human P450
enzymes. The in vitro metabolic pathways Dapagliflozin are
glucuronidation, hydroxylation, and O-deethylation.


Dapagliflozin reduces blood glucose levels by 55% after 0.1 mg/kg oral
dose in hyperglycemic streptozotocin (STZ) rats, which is in part to the
metabolic stability conferred by the C-glucoside linkage. Dapagliflozin
displays a favorable absorption, distribution, Metabolism, and
excretion (ADME) profile and is orally bioavailable. Dapagliflozin (1 mg/kg) causes significant dose-dependent glucosuria and
increase in urine volume in normal rats over 24 hours post-dose.


Dapagliflozin induces increase in urine glucose and urine volume
excretion at 6 hours post-dose in Zucker diabetic fatty (ZDF) rats.
Dapagliflozin lowers fasting and fed glucose levels in ZDF rats even by 2
weeks of treatment, without any marker of renal or liver toxicity.


Dapagliflozin significantly reduces the development of hyperglycaemia,
with lowered blood glucose. Dapagliflozin could improve the insulin
sensitivity, reduce β-cell mass and the development of impaired
pancreatic function.

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