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Submit ReviewDofetilide
说明： KV11.1 (hERG) channel blocker; inhibits rapid delayed rectifier K+ current (IKr)
别名： Tikosyn,UK 68798
化学名： 1-(4-Methanesulphonamidophenoxy)-2-[N-(4-methanesulphonamidophenethyl)-N-methylamino]ethane
纯度： ≥99% (HPLC)
生物活性 for Dofetilide
Dofetilide is a selective potassium channel blocker. Blocks KV11.1 (hERG) channels; inhibits the rapid delayed-rectifier K+ current (IKr). Displays class III antiarrhythmic properties.
许可信息
Sold for research purposes under agreement from Pfizer Inc.
化合物库 for Dofetilide
Dofetilide 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 Dofetilide
| 分子量 | 441.56 |
| 公式 | C19H27N3O5S2 |
| 储存 | Store at RT |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 115256-11-6 |
| PubChem ID | 71329 |
| InChI Key | IXTMWRCNAAVVAI-UHFFFAOYSA-N |
| Smiles | CN(CCC2=CC=C(NS(=O)(C)=O)C=C2)CCOC1=CC=C(NS(=O)(C)=O)C=C1 |
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 Dofetilide
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 44.16 | 100 |
制备储备液 for Dofetilide
以下数据基于产品分子量 441.56。 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 | 2.26 mL | 11.32 mL | 22.65 mL |
| 5 mM | 0.45 mL | 2.26 mL | 4.53 mL |
| 10 mM | 0.23 mL | 1.13 mL | 2.26 mL |
| 50 mM | 0.05 mL | 0.23 mL | 0.45 mL |
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产品说明书 for Dofetilide
参考文献 for Dofetilide
参考文献是支持产品生物活性的出版物。
Gwilt et al (1991) UK-68,798: a novel, potent and highly selective class III antiarrhythmic agent which blocks potassium channels in cardiac cells. J.Pharmacol.Exp.Ther. 256 318 PMID: 1988662
Carmeliet (1992) Voltage- and time-dependent block of delayed K+ current in cardiac myocytes by dofet. J.Pharmacol.Exp.Ther. 262 809 PMID: 1501123
Finlayson et al (2001) [3H]Dofetilide binding in SHSY5Y and HEK293 cells expressing a HERG-like K+ channel. Eur.J.Pharmacol. 412 203 PMID: 11166283
If you know of a relevant reference for Dofetilide, please let us know.
关键词: Dofetilide, Dofetilide supplier, UK68798, hERG, K+, potassium, channels, blockers, inhibits, IKR, delayed, rectifier, currents, Kv, voltage-gated, voltage-dependent, Human, Ether-A-Go-Go, Gene, Pfizer, KV11.1, Tikosyn, UK, 68798, Voltage-Gated, Potassium, Channels, 3757, Tocris Bioscience
5 篇 Dofetilide 的引用文献
引用文献是使用了 Tocris 产品的出版物。 Dofetilide 的部分引用包括：
Mark et al (2020) Reengineering an Antiarrhythmic Drug Using Patient hiPSC Cardiomyocytes to Improve Therapeutic Potential and Reduce Toxicity. Cell Stem Cell 27 813-821.e6 PMID: 32931730
McKeithan et al (2017) An Automated Platform for Assessment of Congenital and Drug-Induced Arrhythmia with hiPSC-Derived Cardiomyocytes. Front Physiol 8 766 PMID: 29075196
Carstensen et al (2019) Effects of UK 68798 and RS 43285 on atrial fibrillatory rate in a horse model of acutely induced atrial fibrillation. J Cardiovasc Electrophysiol 30 596 PMID: 30661267
Roger et al (2017) Drug delivery to the human and mouse uterus using immunoliposomes targeted to the oxytocin receptor. Am J Obstet Gynecol 216 283.e1-283.e14 PMID: 27567564
Bhave et al (2011) Development of a selective small-molecule inhibitor of Kir1.1, the renal outer medullary potassium channel. Mol Pharmacol 79 42 PMID: 20926757
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Dofetilide 的评论
平均评分: 5 (Based on 1 Review.)
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Dofetilide was used to study concentration dependent blocking action on brain Kv channels.
By
Anonymous on 10/31/2018
分析类型： In Vitro
种属： Human
Dofetilide was used to study concentration dependent blocking action on voltage gated potassium channels on human brain cells. Dofetilide showed increasing Kv channel blocking but at high concnetrations the blocking action is hampered.
