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Submit ReviewGlibenclamide
说明： Kir6 (KATP) channel blocker
别名： Glyburide
化学名： 5-Chloro-N-[2-[4-[[[(Cylcohexylamino)carbonyl]amino]sulphonyl]phenyl]ethyl]-2-methoxybenzamide
纯度： ≥99% (HPLC)
生物活性 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.
化合物库 for Glibenclamide
Glibenclamide is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen FDA-Approved Drugs. 了解 Tocris 化合物库的更多信息。
技术数据 for Glibenclamide
| 分子量 | 494 |
| 公式 | C23H28ClN3O5S |
| 储存 | Store at RT |
| 纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for Glibenclamide
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 100 | ||
| ethanol | 5 |
制备储备液 for Glibenclamide
以下数据基于产品分子量 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.
| 浓度/溶剂体积/质量 | 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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产品说明书 for Glibenclamide
参考文献 for Glibenclamide
参考文献是支持产品生物活性的出版物。
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.
关键词: Glibenclamide, Glibenclamide supplier, K+, channel, blockers, KATP, Blocks, CFTR, Cl-, channels, Potassium, KIR, Inward, Rectifier, Chloride, kir6, Glyburide, rectifier, Channels, 0911, Tocris Bioscience
15 篇 Glibenclamide 的引用文献
引用文献是使用了 Tocris 产品的出版物。 Glibenclamide 的部分引用包括：
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
Jiang and Zsombok (2014) Regulation of neurons in the dorsal motor nucleus of the vagus by SIRT1. Front Neurosci 7 270 PMID: 24454277
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
Price et al (2008) Nesfatin-1 inhibits NPY neurons in the arcuate nucleus. Brain Res 1230 99 PMID: 18625211
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
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
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
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
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
O'Malley et al (2020) TRPM4 Conductances in Thalamic Reticular Nucleus Neurons Generate Persistent Firing during Slow Oscillations J Neurosci 40 4813 PMID: 32414784
Seto et al (2013) Acute SimV. inhibits K ATP channels of porcine coronary artery myocytes. J Neurophysiol 8 e66404 PMID: 23799098
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Glibenclamide 的评论
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Glibenclamide prolongs action potential duration in LPS-treated cardiomyocytes.
By
Anonymous on 01/22/2019
分析类型： In Vitro
种属： Other
细胞系/组织： 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
分析类型： In Vivo
种属： 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.
