Ion channel technologies
The importance of the hERG ion channel to drug development and the discovery of the human ion channel genes through the Human Genome Project created significant interest in other ion channel targets. Ion channel dsyfunction has been implicated in diseases and disorders such as cystic fibrosis, diabetes, erectile dysfuncion, epilepsy, heart failure, hypertension, muscular sclerosis, obesity, schizophrenia, and sickle cell anemia. As a result, over 6 billion dollars in yearly sales and 15% of the top selling drugs are targeted for ion channels. In addition, over 500 human ion channel genes have been identified, yet only around 40 have been targeted for therapeutic effects. This suggests that the field of ion channel drug discovery will only increase in the coming years.
Ion channel readers
Applications of the ICR 8000 and ICR 12000 include voltage-gated potassium channels (hERG, Kv1.1, Kv1.4, Kv1.5, SKCa, BKCa), stretch-activated potassium channels, voltage-gated sodium channels (SCN5a, NaV1.2), and tranporters (Na/K-ATPase, K-Cl Co-Transporter).
There are two types of Ion Channel Readers (ICR's)
> The Ion Channel Reader 8000 (ICR-8000)
> The Ion Channel Reader 12000 (ICR-12000)
Ion Channel Reader 8000 (ICR-8000)
The ICR 8000 detects ion channel activity using atomic absorption spectroscopy and flux assays.
Current applications include the evaluation of the hERG potassium channel more quickly, more precisely and more accurately than other medium to high throughput screening systems.
Interactions with the hERG channel can lead to prolonged QT syndrome. Thus, regulatory agencies require the assessment of QT liability.
The ICR 8000 displays broad utility; it can be applied to assess both voltage-gated (hERG, BK/SK, Kv1.1, 1.4, 1.5, KCNQ, 2P,etc.) and ligand-gated (KATP, nAChR, etc.) ion channels.
This allows researchers to accelerate drug development efforts in the treatment and prevention of diseases associated with ion channels.
Benefits:
- Programmable and automated
- Automatic dilution, calibration and cleaning
- Adaptable to existing robotic automation
- Sample dilution not required
- High sensitivity
- On-line dilution
Features:
- Medium Throughput: Up to 5000 wells/day
- Single Channel: Measures 1 sample at a time
- Minimum sample volume: 50 µl
- Accommodation: 96/384-well microplates
- Footprint: H.67 cm X W.55 cm X D.37 cm
- Fuel Source: Acetylene / Compressed Air
- Options: Plate Stacker / Bar Code Reader
- Sensitivity: 0.05 ppm detection limit
- Precision: < 5% CV
Eliminates:
- Quenching effects associated with fluorescence
- Health hazards associated with radioisotopes
- Radioisotope disposal
- Work restrictions posed by Rb's short half-life
- Ideal for hERG channel assays.
Ion Channel Reader 12000 (ICR-12000)
The ICR 12000 designed for ultra high throughput screening of compound libraries against ion channel targets.
Based on the robustness of Aurora Biomed's ICR technology, the reader offers high sensitivity generating accurate drug rank order matching electrophysiology data.
This new member of the ICR series provides the throughput to access compound QT liability early in the drug discovery process.
Technology:
The technology is based upon the versatility, precision, and sensitivity of atomic absorption spectroscopy (AAS) and Aurora Biomed's patented microsampling process. Ion Channel Technology is suitable for both ligand-gated and voltage-gated ion channels using cell-based flux assays.
Features:
- High Throughput: Up to 60,000 wells/day
- Multi-Channel: Measures 12 samples at a time
- Minimum sample volume: 20 µl
- Accommodation: 96/384-well microplates
- Footprint: H.135 cm X W.134cm X D.97cm
- Fuel Source: Natural Gas / Compressed Air
- Includes: Plate Stacker / Bar Code Reader
- Sensitivity: 0.05 ppm detection limit
- Precision: < 5% CV
Applications :
Channel Reader technology is suitable for many types of ion channels broad applications include:
- Shaker (Kv1.1, Kv1.4 and Kv1.5)
- hERG
- KCNQ4
- B/SKCa
- KCNB/TASK-3
- Kir2.1
- nAChR
- KATP (P2X family)