Glyburide-d3 (Synonyms: Glibenclamide-d3)

Glyburide-d₃ is intended for use as an internal standard for the quantification of glyburide by GC- or LC-MS. Glyburide is a sulfonylurea and an inhibitor of sulfonylurea receptor 1 (SUR1) linked to ATP-sensitive potassium channel K_ir6.2 (IC₅₀ = 4.3 nM).¹ It binds to microsomes derived from RINm5F pancreatic β-cells (K_d = 0.3 nM) and inhibits ⁸⁶Rb⁺ efflux from intact RINm5 cells with a half-maximal inhibition (K_0.5) value of 0.06 nM.² Glyburide (5 mg/kg) reduces blood glucose levels and increases the activity of hepatic glutathione-S-transferase (GST) and glucose-6-phosphate dehydrogenase (G6PDH) in a rat model of diabetes induced by streptozotocin .³ It inhibits ATP-induced increases in caspase-1 activation and IL-1β and IL-18 secretion in a concentration-dependent manner in LPS-primed bone marrow-derived macrophages (BMDMs).⁴ Glyburide (80 mg/ml) also reduces lesion growth in mice infected with L. mexicana.⁵ Formulations containing glyburide have been used in the treatment of type 2 diabetes.

1.Coghlan, M.J., Carroll, W.A., and Gopalakrishnan, M.Recent developments in the biology and medicinal chemistry of potassium channel modulators: Update from a decade of progressJ. Med. Chem.44(11)1627-1653(2001) 2.Schmid-Antomarchi, H., De Weille, J., Fosset, M., et al.The receptor for antidiabetic sulfonylureas controls the activity of the ATP-modulated K+ channel in insulin-secreting cellsThe Journal of Biological Chemisty262(33)15840-15844(1987) 3.Bugdayci, G., Altan, N., Sancak, B., et al.The effect of the sulfonylurea glyburide on glutathione-S-transferase and glucose-6-phosphate dehydrogenase in streptozotocin-induced diabetic rat liverActa. Diabetol.43(4)131-134(2006) 4.Lamkanfi, M., Mueller, J.L., Vitari, A.C., et al.Glyburide inhibits the Cryopyrin/Nalp3 inflammasomeJournal of Cell Biology187(1)61-70(2009) 5.Serrano-MartÍn, X., Payares, G., and Mendoza-LeÓn, A.Glibenclamide, a blocker of K+ATP channels, shows antileishmanial activity in experimental murine cutaneous leishmaniasisAntimicrobial Agents and Chemotherapy50(12)4214-4216(2006)