Glyburide-d 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 K6.2 (IC = 4.3 nM). It binds to microsomes derived from RINm5F pancreatic β-cells (K = 0.3 nM) and inhibits Rb efflux from intact RINm5 cells with a half-maximal inhibition (K) value of 0.06 nM. 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 (STZ; ). 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). Glyburide (80 mg/ml) also reduces lesion growth in mice infected with L. mexicana. Formulations containing glyburide have been used in the treatment of type 2 diabetes.
Glyburide-d3 is the deuterium labeled Glibenclamide. Glibenclamide (Glyburide) is an orally active ATP-sensitive K+ channel (KATP) inhibitor and can be used for the research of diabetes and obesity. Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR). Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability. Glibenclamide can induce autophagy.
分子式
C23H25ClD3N3O5S
分子量
497.02252
CAS号
1219803-02-7
中文名称
格列本脲-D3氘代内标
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
6 months
-20°C
1 month
溶解性数据
In Vitro:
DMSO: 100 mg/mL (201.20 mM; Need ultrasonic)
H2O: 0.1 mg/mL (0.20 mM; Need ultrasonic and warming)