Dapagliflozin (2S)-1,2-propanediol hydrate is a potent, selective, orally active hSGLT2 inhibitor with EC50 of 1.12 nM.
Dapagliflozin displays >300-fold selectivity over hSGLT1 (EC50=330 nM), highly selectivity versus GLUT transporters.
Dapagliflozin also is a potent selective inhibitor of rSGLT2 (EC50=3 nM), with 200-fold selectivity versus rSGLT1.
Dapagliflozin significantly improves glucose homeostasis, reduces blood glucose levels in hyperglycemic streptozotocin (STZ) rats.
Physicochemical Properties
M.Wt
502.9823
Formula
C24H35ClO9
Appearance
Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility
10 mM in DMSO
Chemical Name/SMILES
D-Glucitol, 1,5-anhydro-1-C-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-, (1S)-, compd. with (2S)-1,2-propanediol, hydrate (1:1:1)
References
1. Meng W, et al. J Med Chem. 2008 Mar 13;51(5):1145-9.
2. Han S, et al. Diabetes. 2008 Jun;57(6):1723-9.
3. Wilson C. Nat Rev Endocrinol. 2010 Oct;6(10):531.
4. Komoroski B, et al. Clin Pharmacol Ther. 2009 May;85(5):513-9.
