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Cat. No. Name Size Price Add Cart
KI0500BMS5121458QuoteQuote

Chemical Characteristic

Product NameBMS5121458
SynonymsDapagliflozin, Forxiga
CAS No.461432-26-8
Molecular Weight 408.87
FormulaC21H25ClO6
Chemical Name(2S,3R,4R,5S,6R)-2-(3-(4-ethoxybenzyl)-4-chlorophenyl)-6-(hydroxymethyl)-tetrahydro-2H-pyran-3,4,5-triol
Smiles[C@@H]1([C@@H]([C@H]([C@@H]([C@H](O1)CO)O)O)O)c1cc(c(cc1)Cl)Cc1ccc(cc1)OCC
Chemical Structure

Biological activities

BMS512148 is a potent, selective renal sodium-dependent glucose cotransporter 2 (SGLT2) inhibitor.[1] The IC50 of BMS512148 is 0.49 nM against SGLT2.[2] BMS512148 prevents the reabsorption of glucose at the renal proximal tubule. BMS512148 produces a sustained, dose-dependent reduction in plasma glucose levels while simultaneously improving insulin secretion and sensitivity.[3] BMS512148 potently and selectively inhibits human SGLT2 versus human SGLT1, the major cotransporter of glucose in the gut. BMS512148 inhibits human SGLT2 and rat SGLT2 with EC50 of 1.1 and 3 nM, respectively. In contrast, BMS512148 inhibits human SGLT1 and rat SGLT1 with EC50 of 1.39 and 0.62 μM, respectively.[4] In vivo, BMS512148 acutely induces renal glucose excretion in normal and diabetic rats. BMS512148 improves glucose tolerance in normal rats. BMS512148 reduces hyperglycemia in Zucker diabetic fatty (ZDF) rats after single oral doses ranging from 0.1 to 1.0 mg/kg. Once-daily BMS512148 treatment over 2 weeks significantly lowers fasting and fed glucose levels at doses ranging from 0.1 to 1.0 mg/kg. BMS512148 significantly increases in glucose utilization rate accompanied by a significant reduction in glucose production. When measured 24 hours after the final dose on day 15, ZDF rats treated with 0.5 mg/kg BMS512148 reveals a 53% decrease in 18-hour FPG level compared with vehicle-treated rats [4] In the dog, the systemic blood clearance of BMS512148 is 2.5, which is ∼8% of hepatic blood flow in the dog. In the monkey, dapagliflozin is cleared more quickly than in the dog, with a systemic blood clearance of 8.8 mL/min/kg, approximately 20% of hepatic blood flow in the monkey.[5]

Protocols

BMS512148 is dissolved in dimethyl sulfoxide (DMSO).[5]

References

[1] Meng W, et al. Discovery of dapagliflozin: a potent, selective renal sodium-dependent glucose cotransporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes. J Med Chem. 2008, 51(5): 1145-1149.
[2] Lee J, et al. Pyrimidinylmethylphenyl glucoside as novel C-aryl glucoside SGLT2 inhibitors. Bioorg Med Chem Lett. 2010, 20(23): 7046-7049.
[3] Shah NK, et al. Dapagliflozin: a novel sodium-glucose cotransporter type 2 inhibitor for the treatment of type 2 diabetes mellitus. Pharmacotherapy. 2012, 32(1): 80-94.
[4] Han S, et al. Dapagliflozin, a selective SGLT2 inhibitor, improves glucose homeostasis in normal and diabetic rats. Diabetes. 2008, 57(6): 1723-1729.
[5] Obermeier M, et al. In vitro characterization and pharmacokinetics of dapagliflozin (BMS-512148), a potent sodium-glucose cotransporter type II inhibitor, in animals and humans. Drug Metab Dispos. 2010, 38(3): 405-414.

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