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Glyburide-d3
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Glyburide-d3图片
CAS NO:1219803-02-7
包装与价格:
包装价格(元)
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An internal standard for the quantification of glyburide
Cas No.1219803-02-7
别名优降糖D3,Glyburide-d3
Canonical SMILESClC1=CC(C(NCCC2=CC=C(S(NC(NC3CCCCC3)=O)(=O)=O)C=C2)=O)=C(OC([2H])([2H])[2H])C=C1
分子式C23H25ClD3N3O5S
分子量497
溶解度DMSO: Soluble
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Glyburide-d3is 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 Kir6.2 (IC50= 4.3 nM).1It binds to microsomes derived from RINm5F pancreatic β-cells (Kd= 0.3 nM) and inhibits86Rb+efflux from intact RINm5 cells with a half-maximal inhibition (K0.5) value of 0.06 nM.2Glyburide (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 .3It 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).4Glyburide (80 mg/ml) also reduces lesion growth in mice infected withL. mexicana.5Formulations 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)

 
 
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