| Name | Glibenclamide |
| Description | Glibenclamide (Glyburide) is an antidiabetic sulfonylurea derivative with actions similar to those of chlorpropamide. |
| In vitro | Administered intravenously at a dose of 25 mg/kg, Glyburide increased sodium (Na) ion excretion by 350% one hour after treatment, without affecting potassium (K) ion excretion, glomerular filtration rate, mean arterial pressure, or heart rate. In awake rats subjected to a saline load, Glyburide dose-dependently increased urinary sodium excretion, while urinary potassium excretion remained largely unchanged. |
| In vivo | Glyburide enhances the apparent affinity of scavenger receptor class B type I (SR-BI) for high-density lipoprotein (HDL) binding in insulin-secreting cells. It inhibits SR-BI-mediated selective lipid uptake and efflux, with potency similar to its inhibition of ABCA1 (IC50 approximately 275-300 mM). Regardless of the pre-existing relaxation level, Glyburide can also reverse the relaxation induced by pinacidil. At a concentration of 0.03 mM, Glyburide blocks ATP-modulated potassium channels in insulin-secreting cells. It causes a concentration-dependent increase in the IC50 values for BRL34915 and diazoxide, eliminating the relaxation response to minoxidil sulfate. Doses of Glyburide ranging from 10-500 nM proportionately inhibit the relaxation time brought about by potassium channel openers. |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 99 mg/mL (200.4 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
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| Keywords | Cystic fibrosis transmembrane conductance regulator | Inhibitor | Multidrug resistance protein 1 | CFTR | Glibenclamide | fibrosis | regulator | bioenergetics | Cluster of differentiation 243 | inhibit | mitochondrial | cystic | Mitochondrial Metabolism | KcsA | conductance | MDR1 | Autophagy | adipocytes | Pgp | P-glycoprotein | CD243 | ABCB1 | SUR1 | obesity | transmembrane | ATP-sensitive | diabetes | P-gp | Potassium Channel |
| Inhibitors Related | Hydroxychloroquine | Guanidine hydrochloride |
| Related Compound Libraries | Membrane Protein-targeted Compound Library | EMA Approved Drug Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library | FDA-Approved Drug Library | Anti-Aging Compound Library | Ion Channel Targeted Library |
United States
