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G0639 Sigma-Aldrich

Glybenclamide

≥99% (HPLC)

Synonym: 5-Chloro-N-[4-(cyclohexylureidosulfonyl)phenethyl]-2-methoxybenzamide, Glyburide, N-p-[2-(5-Chloro-2-methoxybenzamido)ethyl]benzenesulfonyl-N′-cyclohexylurea

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Properties

Related Categories Approved Therapeutics/Drug Candidates, Bioactive Small Molecule Alphabetical Index, Bioactive Small Molecules, Cell Biology, Cell Signaling and Neuroscience,
InChI Key   ZNNLBTZKUZBEKO-UHFFFAOYSA-N
assay   ≥99% (HPLC)
solubility   ethanol: 2 mg/mL
  DMSO: soluble
  H2O: insoluble
originator   Roche
storage temp.   2-8°C
Gene Information   human ... KCNH2(3757), KCNJ1(3758), KCNJ11(3767)
rat ... Kcnj1(24521)

Description

Application

Glybenclamide has been used:
• as a positive control oral hypoglycemic drug to study the hypoglycemic effects of Chlorella in streptozotocin-induced diabetic mice
• as a K+ATP channel antagonist in canine with induced acute hypoxia
• as an inhibitor of cystic fibrosis transmembrane conductance regulator (CFTR) channel in fetal distal lung epithelial (FDLE) cells

Packaging

5, 10 g in poly bottle

Biochem/physiol Actions

Glybenclamide is a sulfonylurea class of antidiabetic drug used in the treatment of type 2 diabetes mellitus. It has benzamide moiety and stimulates pancreatic β cells to produce insulin resulting in a hypoglycemic effect. It selectively blocks ATP-sensitive K+ channels in the brain with high-affinity binding sites and elicits cardiovascular effects. It may be a potential therapeutic for thromboembolic disorders due to its in vivo antiplatelet functionality. Glybenclamide traverses to the ischemic brain and provides neuroprotection especially during the early stages of stroke.

Selectively blocks ATP-sensitive K+ channels; high affinity binding sites found in brain, pancreatic β cells, and cardiovascular system.

Features and Benefits

This compound is a featured product for ADME Tox research. Click here to discover more featured ADME Tox products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

This compound is also offered as part of Sigma′s Library of Pharmacologically Active Compounds (LOPAC®1280), a biologically annotated collection of high-quality, ready-to-screen compounds. Click here to learn more.

This compound is featured on the Chloride Channels and Potassium Channels pages of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

This compound was developed by Roche. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Legal Information

LOPAC is a registered trademark of Sigma-Aldrich Co. LLC

Safety & Documentation

Safety Information

RIDADR 
NONH for all modes of transport
WGK Germany 
2
RTECS 
YS4725200

Documents

Certificate of Analysis (COA)

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Certificate of Origin (COO)

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Protocols & Articles

Articles

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Ion transport across the relatively impermeable lipid bilayer of the cell membrane is accomplished via membrane proteins known as ion channels, pumps and transporters. Ion channels are gated pores an...
Keywords: Biological processes, Cell signaling, Diseases, Hormones, Ligands, Neurotransmitters

Peer-Reviewed Papers
15

References

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