离子通道筛选细胞株
欧罗拉可提供最普遍的药物研发的离子通道靶点细胞株,以供购买以及许可认证用途。包括稳定表达hERG钾离子通道细胞株,Kv1.3钾离子通道细胞株,或者Nav1.5钠离子通道细胞株,每种细胞株均经过优化,适用于离子析出分析以及电生理分析。这些细胞株测试窗口(信号/噪音)适用于高通量筛选。配合欧罗拉的离子通道阅读器系列以及优化的试剂,能够得到稳定、灵敏的离子通道筛选分析结果。
索取资料hERG细胞株
药物引发的人类ether-a-go-go (hERG)钾离子通道抑制与QT间期延长有关,QT间期延长可导致心律不齐,例如尖端扭转型室性心动过速。因此,在药物研发过程化合物早期筛选中,对hERG通道活性影响测试的显得尤为重要。我司CHO-hERG细胞株是专门针对可导致QT间期延长的化合物筛选而研发:
- 稳定表达hERG钾离子通道
- 已证实适用于电生理以及离子析出分析
- 适用于高通量筛选(HTS)
Kv1.3 钾离子通道细胞株
Kv1.3钾离子通道已经证实可作为某些药物治疗靶点,例如多发性硬化、肥胖症以及其他相关疾病。为了获得Kv1.3离子通道拮抗的化合物筛选库,需要一个稳定可靠的表达系统。欧罗拉的CHO-Kv1.3钾离子通道细胞株可高水平表达Kv1.3通道,随着时间推移也不会影响表达的稳定性。该细胞株:
- 稳定表达Kv1.3钾离子通道
- 已证实适用于电生理以及离子析出分析
- 适用于高通量筛选(HTS)
相关论文:
Nav1.5 钠离子通道细胞株
心肌细胞的钠离子通道Nav1.5,也称为hH1a,是一种重要的心脏毒性筛选的靶点,因为该离子通道编码基因(SCN5a)的变异,可引起长QT综合征(LQT3)。由于该变异引起的心律不齐相对于LQT1 (KVLQT1) 或 LQT2 (hERG)更容易致命。而且,该离子通道的非特异性药物结合可导致不正常的心率不整。因此,Nav1.5测试被纳入到心脏毒性筛选项目中。对于新型化学实体的Nav1.5离子通道活性测试早期筛选,是药物研发过程中非常重要一环。我司的HEK-Nav1.5的钠离子通道细胞株是专为诸如新型化学实体(NCEs)筛选而研发,该类钠离子通道细胞株:
- 稳定表达Nav1.5钠离子通道
- 已证实适用于电生理以及离子析出分析
- 适用于高通量筛选 (HTS)
资料下载:离子通道筛选细胞株
Applications
Publications
- • Nonradioactive Rubidium Efflux Assay Technology for Screening of Ion Channels(Georg C. Terstappen)
- • Ion Flux and Ligand Binding Assays for Analysis of Ion Channels(Georg C. Terstappen)
- • Development and validation of HTS assay for screening the calcium-activated chloride channel modulators in TMEM16A stably expressed CHO cells
- • Screening technologies for ion channel drug discovery
- • Analogs of MK-499 are differentially affected by a mutation in the S6 domain of the hERG K+ channel
- • High-throughput analysis of drug binding interactions for the human cardiac channel, Kv1.5
- • Cellular HTS Assays for Pharmacological Characterization of Na V 1.7 Modulators
- • Zinc pyrithione-mediated activation of voltage-gated KCNQ potassium channels rescues epileptogenic mutants
- • Evaluation of the Rubidium Efflux Assay for Preclinical Identification of hERG Blockade
- • Characterization of a hERG Screen Using the IonWorks HT: Comparison to a hERG Rubidium Efflux Screen
- • Development of an HTS Assay for Na , K -ATPase Using Nonradioactive Rubidium Ion Uptake
- • Rb + Flux through hERG Channels Affects the Potency of Channel Blocking Drugs: Correlation with Data Obtained Using a High-Throughput Rb + Efflux Assay
- • Atomic Absorption Spectroscopy in Ion Channel Screening
- • Nonradioactive Rubidium Ion Efflux Assay and Its Applications in Drug Discovery and Development
- • Validation of an Atomic Absorption Rubidium Ion Efflux Assay for KCNQ/M-Channels Using the Ion Channel Reader 8000
- • High Throughput Assay Technologies for Ion Channel Drug Discovery
- • A High Throughput Screening Techno logy-Overcoming Bottlenecks in Ion Channel Drug Targets
- • A medium-throughput functional assay of KCNQ2 potassium channels using rubidium efflux and atomic absorption spectrometry