| 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/Shipping at ambient temperature. |
| Solubility Information | DMSO : 99 mg/mL (200.4 mM), Sonication is recommended.
H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.3 mg/mL (6.68 mM), Sonication is recommended.
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| Keywords | transmembrane | SUR1 | regulator | PotassiumChannel | Potassium Channel | P-gp (P-glycoprotein) | P-gp | Pgp | P-glycoprotein | obesity | Multidrug resistance protein 1 | MitochondrialMetabolism | Mitochondrial Metabolism | mitochondrial | MDR1 | KcsA | Inhibitor | inhibit | Glibenclamide | fibrosis | diabetes | Cystic fibrosis transmembrane conductance regulator | cystic | conductance | Cluster of differentiation 243 | CFTR | CD243 | bioenergetics | Bile salt export pump | Autophagy | ATP-sensitive | adipocytes | ABCB1 |
| Inhibitors Related | Stavudine | Aceglutamide | Cysteamine hydrochloride | Sodium 4-phenylbutyrate | Hydroxychloroquine | Guanidine hydrochloride | 1,8-Cineole | Paeonol | Sodium butanoate | Naringin | Alginic acid | Gefitinib |
| Related Compound Libraries | Pain-Related Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | EMA Approved Drug Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library | FDA-Approved Drug Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Ion Channel Targeted Library | Anti-Cancer Drug Library |
United States
