Glibenclamide

SKU: orb1307954

Description

Glibenclamide

Research Area

Cell Biology, Metabolism Research, Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 10238-21-8
• MW: 494.00
• Purity: 99.56%
• Formula: C₂₃H₂₈ClN₃O₅S
• SMILES: C(NCCC1=CC=C(S(NC(NC2CCCCC2)=O)(=O)=O)C=C1)(=O)C3=C(OC)C=CC(Cl)=C3
• Target: Mitochondrial Metabolism,CFTR,Potassium Channel,P-gp,Autophagy
• Solubility: Ethanol:< 1 mg/mL (insoluble or slightly soluble);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:260 mg/mL (526.32 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (6.68 mM)

Bioactivity

• 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.
• 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.

Storage & Handling

• 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.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SUR1, regulator, P-glycoprotein, Pgp, P-gp, P-gp (P-glycoprotein), Potassium Channel, PotassiumChannel, transmembrane, obesity, MitochondrialMetabolism, Mitochondrial Metabolism, mitochondrial, KcsA, Inhibitor, Multidrug resistance protein 1, inhibit, MDR1, fibrosis, Glyburide, Glibenclamide, conductance, Cluster of differentiation 243, CFTR, CD243, Cystic fibrosis transmembrane conductance regulator, cystic, diabetes, Bile salt export pump, bioenergetics, Autophagy, ATP-sensitive, ABCB1, adipocytes

Compound Identifiers

PubChem CID

3488