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Submit ReviewGlibenclamide
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)
Biological Activity for Glibenclamide
Glibenclamide is an 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 for Glibenclamide
Glibenclamide is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen FDA-Approved Drugs. Find out more about compound libraries available from Tocris.
Technical Data for Glibenclamide
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Glibenclamide
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 100 | ||
| ethanol | 5 |
Preparing Stock Solutions for Glibenclamide
The following data is based on the product molecular weight 494. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 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 |
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Product Datasheets for Glibenclamide
References for Glibenclamide
References are publications that support the biological activity of the product.
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.
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Keywords: Glibenclamide, Glibenclamide supplier, K+, channel, blockers, KATP, Blocks, CFTR, Cl-, channels, Potassium, KIR, Inward, Rectifier, Chloride, kir6, Glyburide, rectifier, Channels, 0911, Tocris Bioscience
15 Citations for Glibenclamide
Citations are publications that use Tocris products. Selected citations for Glibenclamide include:
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
Lee et al (2011) Role of perivascular adipose tissue-derived methyl palmitate in vascular tone regulation and pathogenesis of hypertension. Circulation 124 1160 PMID: 21844078
O'Malley et al (2020) TRPM4 Conductances in Thalamic Reticular Nucleus Neurons Generate Persistent Firing during Slow Oscillations J Neurosci 40 4813 PMID: 32414784
Xu (2012) Effect of the ginsenoside Rb1 on the spontaneous contraction of intestinal smooth muscle in mice. World J Gastroenterol 18 5462 PMID: 23082064
Parsons (2010) ATP-sensitive potassium channel-mediated lactate effect on orexin neurons: implications for brain energetics during arousal. J Neurosci 30 8061 PMID: 20554857
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
Chung et al (2011) Expression and functional properties of TRPM2 channels in DArgic 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
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
Seto et al (2013) Acute SimV. inhibits K ATP channels of porcine coronary artery myocytes. J Neurophysiol 8 e66404 PMID: 23799098
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
Jiang and Zsombok (2014) Regulation of neurons in the dorsal motor nucleus of the vagus by SIRT1. Front Neurosci 7 270 PMID: 24454277
Price et al (2008) Nesfatin-1 inhibits NPY neurons in the arcuate nucleus. Brain Res 1230 99 PMID: 18625211
Mehmood et al (2015) Antidiarrhoeal, antisecretory and antispasmodic activities of Matricaria chamomilla are mediated predominantly through K(+)-channels activation. Neuroscience 15 75 PMID: 25886126
Fransen et al (2015) Dissecting out the complex Ca2+-mediated phenylephrine-induced contractions of mouse aortic segments. Biomed Res Int 10 e0121634 PMID: 25803863
Do you know of a great paper that uses Glibenclamide from Tocris? Please let us know.
Reviews for Glibenclamide
Average Rating: 5 (Based on 2 Reviews.)
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Glibenclamide prolongs action potential duration in LPS-treated cardiomyocytes.
By
Anonymous on 01/22/2019
Assay Type: In Vitro
Species: Other
Cell Line/Tissue: Ventricular cardiomyocytes
Primary guinea pig ventricular cardiomyocytes were incubated with LPS for 6-10 h. Cells were patched and stimulated at a 1 Hz frequency. Action potentials were recorded before and after glibenclamide (5 microM) containing normal tyrode solution. Glibenclamide prolonged action potential duration in LPS-treated cardiomyocytes; indicating role of KATP channels.
Glibenclamide was used to study combination drug effect with B blockers.
By
Anonymous on 10/29/2018
Assay Type: In Vivo
Species: Mouse
Glibenclamide was used in our lab to study combination drug effect. Beta blocker and glibenclamide was administered in combination and separately to study their pattern of action over blood glucose level.
