Glibenclamide

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Cat.No. 0911 - Glibenclamide | C23H28ClN3O5S | CAS No. 10238-21-8
Description: Kir6 (KATP) channel blocker
Alternative Names: Glyburide
Chemical Name: 5-Chloro-N-[2-[4-[[[(Cylcohexylamino)carbonyl]amino]sulphonyl]phenyl]ethyl]-2-methoxybenzamide
Purity: ≥99% (HPLC)
Datasheet
Citations (11)
Literature

Biological Activity

ATP-dependent K+ channel (Kir6, KATP) and CFTR Cl- channel blocker. Inhibits Kir6 currents in the pancreas, causing an increase in intracellular Ca2+ and insulin secretion. Inhibits recombinant CFTR Cl- channels with an IC50 of 20 μM.

Compound Libraries

Glibenclamide is also offered as part of the Tocriscreen Plus and Tocriscreen Library of FDA-Approved Compounds. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 494
Formula C23H28ClN3O5S
Storage Store at RT
Purity ≥99% (HPLC)
CAS Number 10238-21-8
PubChem ID 3488
InChI Key ZNNLBTZKUZBEKO-UHFFFAOYSA-N
Smiles COC1=C(C=C(Cl)C=C1)C(=O)NCCC1=CC=C(C=C1)S(=O)(=O)NC(=O)NC1CCCCC1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

SolubilitySoluble to 100 mM in DMSO and to 5 mM in ethanol

Preparing Stock Solutions

The following data is based on the product molecular weight 494. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.02 mL 10.12 mL 20.24 mL
5 mM 0.4 mL 2.02 mL 4.05 mL
10 mM 0.2 mL 1.01 mL 2.02 mL
50 mM 0.04 mL 0.2 mL 0.4 mL

Molarity Calculator

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

Brogden et al (1979) Glibenclamide: a review. Drugs 18 329 PMID: 389600

Robertson et al (1990) Potassium channel modulators: scientific applications and therapeutic promise. J.Med.Chem. 33 1529 PMID: 2187993

Sheppard and Welsh (1992) Effect of ATP-sensitive K+ channel regulators on cystic fibrosis transmembrane conductance regulator chloride channels. J.Gen.Physiol. 100 573 PMID: 1281220


If you know of a relevant reference for Glibenclamide, please let us know.

View Related Products by Product Action

View all Inward Rectifier Potassium (Kir) Channel Blockers

Keywords: K+ channel blockers KATP Blocks CFTR Cl- channels Potassium KIR Inward Rectifier Chloride kir6 Glyburide Inward rectifier Potassium Channels

11 Citations for Glibenclamide

Citations are publications that use Tocris products. Selected citations for Glibenclamide include:

Quock et al (2011) The acute antinociceptive effect of HBO2 is mediated by a NO-cyclic GMP-PKG-KATP channel pathway in mice. Brain Res 1368 102 PMID: 20977894

Chung et al (2011) Expression and functional properties of TRPM2 channels in dopaminergic neurons of the substantia nigra of the rat. J Korean Med Sci 106 2865 PMID: 21900507

Saloman et al (2011) Activation of peripheral δ-opioid receptors leads to anti-hyperalgesic responses in the masseter muscle of male and female rats. PLoS One 190 379 PMID: 21664434

He et al (2010) Inflammation and fibrosis during Chlamydia pneumoniae infection is regulated by IL-1 and the NLRP3/ASC inflammasome. J Immunol 184 5743 PMID: 20393140

Song et al (2010) Polyphenol (-)-epigallocatechin gallate during ischemia limits infarct size via mitochondrial K(ATP) channel activation in isolated rat hearts. PLoS One 25 380 PMID: 20191036

Price et al (2008) Nesfatin-1 inhibits NPY neurons in the arcuate nucleus. Brain Res 1230 99 PMID: 18625211

Fransen et al (2015) Dissecting out the complex Ca2+-mediated phenylephrine-induced contractions of mouse aortic segments. Biomed Res Int 10 e0121634 PMID: 25803863

Mehmood et al (2015) Antidiarrhoeal, antisecretory and antispasmodic activities of Matricaria chamomilla are mediated predominantly through K(+)-channels activation. Neuroscience 15 75 PMID: 25886126

Jiang and Zsombok (2014) Regulation of neurons in the dorsal motor nucleus of the vagus by SIRT1. Front Neurosci 7 270 PMID: 24454277

Chen et al (2014) Characterization of imidazoline receptors in blood vessels for the development of antihypertensive agents. J Pharmacol Exp Ther 2014 182846 PMID: 24800210

Seto et al (2013) Acute simvastatin inhibits K ATP channels of porcine coronary artery myocytes. J Neurophysiol 8 e66404 PMID: 23799098


Do you know of a great paper that uses Glibenclamide from Tocris? If so please let us know.

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Pathways for Glibenclamide

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