Qube Opto 384 – for optical stimulation of ion channels or compounds.

Optical stimulation combined with Automated Patch Clamp allows for precise control of e.g. channelrhodopsins, caged compounds and pacing studies. To allow for even better control than with our standard APC solutions, we have now integrated 384 adjustable LEDs to allow for optical stimulation of ion channels, ligands or compounds.

To compensate for heating due to the large amount of energy released, we have adapted our on-site temperature control, so temperature effects are reduced to a minimum.

To avoid desensitization from ambient light we have darkened the cabinet so Qube looks even cooler, having a distant resemblance to a well-known character from a movie happening in a galaxy far, far away.

• 384 LEDs to ensure consistent and even light distribution throughout all 384 sites
• Light ramps and other waveforms through adjustment of timing, duration and intensity of light
• Integrated temperature control to avoid unwanted temperature effect
• Full LED control integrated in Qube software
• Dark cabinet allows for automated handling of light sensitive compounds and cells

During the coming months we will be playing with this new setup ourselves together with a few select partners. If you are also interested to discover the full potential of this setup and would like to come play with us, you are welcome to contact Sandra Wilson (swi@sophion.com) or visit booth #518 at Biophysics for more information.

High throughput screening on Nav1.1 using Qube

The voltage-gated sodium channel Na_V1.1 is highly expressed in fast spiking interneurons (FSIs), which are important for memory encoding and other cognitive functions. An impaired function of FSIs is associated with disorders like autism, schizophrenia, Alzheimer’s and others. Potentiators of Na_V1.1 have been shown to minimize cognitive dysfunction in transgenic mice with decreased levels of Na_V1.1 in parvalbumin-positive neurons and this target thus lend itself to therapeutic intervention. The challenge is to identify the molecule with the desired mode-of-action which inherently requires electrophysiology. In summary we show that Qube 384 provides:

• Success rates up to 97%
• Stable, unattended measurements over 7 hours
• Consistent current voltage relationship
• High reliability of detecting Na_V1.1 activators

For the full application report please see here.

Welcome to our new field service engineer, Thomas Byrne

To ensure our customers continue to get the best service, especially with the increasing number of instrument purchases in North America, we are staffing up our Service Operation.

Thomas Byrne comes to Sophion from Olympus Scientific Solutions Americas where he was a systems engineer supporting clients worldwide onsite and remotely. He also worked as a Senior Field Service Engineer at Hospira Worldwide Inc supporting their products and services to hospitals in the Northeast.

We are very excited to have Thomas on board, and together with Lars Maul the two of them will continue to provide the best in class service to our customers as our business continues to grow.

Japanese Safety Pharmacology Society 9th Annual Meeting

We look forward to JSPS 9^th annual meeting at The University of Tokyo, Yayoi Auditorium. You can find the entire program here.

You can meet with our ion channel experts at our booth #I at the Yayoi Auditorium. We are participating in the stamp rally.

Poster Presentation

On Saturday, 10th February between 11.30 AM and 12.30 PM, Dr. Kazuya Tsurudome will present a poster titled:

Voltage and current clamp recordings from human iPS cell-derived cardiomyocytes on 384-channel automated patch-clamp system

Poster board no. 16

A list of all poster presented at JSPS can be found here.

Virtual Qube – Increase value from your CRO data

A Contract Research Organization will supply you with reports of your data. But in case you are interested in digging deeper into the immense value contained in high fidelity recordings from Qube, you can benefit for Qube External Data server solution.

Qube External Data server enables all the analysis needed to evaluate the results, from raw current traces, via current-time plots to Hill-fits of pharmacological effects or estimation of voltage of half maximal inactivation found on the Boltzmann-curve. If you want to export data e.g. to an inhouse database, this is also possible at all levels of data-maturity.

In case you have your own Qube, the analysis part is familiar and the use of the external data server could be segmenting large portions of data as well as release space on the internal data drive in Qube when that starts to fill up…however, we supply Qube with 8 TB memory and intelligent data reduction so it can take a while but good to know that it still shouldn’t limit you.

The Virtual Qube comes with two years free upgrade of Sophion software.

SLAS2018

This year you can meet the following Sophion people:

• Richard Kondo, sales manager, North America
• Weifeng Yu, director of customer support, North America
• Daniel Sauter, applications scientist, North America
• Thomas Binzer, vice president – R&d & Marketing

On Wednesday, February 7, 2018, 11:30 AM – 12:30 PM Daniel Sauter will be presenting a poster titled (Poster Number 1319-E-):

HT Automation for patch clamp based primary screen for Na_V1.1 using Qube384

Read more about SLAS2018 here.

hCav1.2 recordings on Qube 384 using step, train and CiPA protocols

Some ion channels have a tendency to exhibit reducing current level in the course of an experiment. A notable member of this class is the Ca_V1.2 channel, a very important ion channel expressed in nervous tissue, the heart and smooth muscle and thus a target for a range of therapeutics as well as a liability target for other groups of medications. Therefore it is important to be able to record reliably, stably and with a high success rate in the pursue of novel compounds with the desired profile on Ca_V1.2 modulation. Qube 384 provides a stable assay with the Ca_V1.2 channel generated by SB Drug Discovery with these characteristics:

• Pharmacology and current-voltage relationship in accordance with literature values
• Success rates up to 94%
• Stable currents with rundown as low as (1.2 ± 0.9)% per minute
• The CiPA protocol yields stable currents with rundown as low as (1 ± 1)% per minute

For the full application report please see here.

Note that we have another Qube Application Report on Cav1.2 on another commercially available cell line underlining the robustness of the Qube platform. Find both of them here

For more information please contact info@sophion.com

Biophysics 2018 – here we come!

Time flies and soon BPS2018 will kick-off in San Francisco. We look forward to see you in San Francisco and hope that you will join us for the below events:

• Satellite meeting – Friday, February 16th
• Beer tasting and dining – Saturday, February 17th
• Sophion Ion Channel meeting – Tuesday, February 20th
• Poster presentation – Wednesday, February 21st

Read much more about each event here and make sure to sign up as the seats fill up quickly.

2017 in brief

What a year!

For Sophion it has been a year with many changes, a lot of news and countless achievements. It has also, by far, been the best year in the history of Sophion Bioscience and on behalf of the whole Sophion Bioscience team we would like to thank all our partners and customers for their continued support. Read more about 2017 seen from our perspective here “Sophion 2017 in brief”

Happy New Year

We look very much forward to working with both new and old customers in 2018.

Sophion User Meeting, Boston – Save the date!

We are still working with the agenda but can, at this point, reveal that we have the pleasure of having Julie Klint, Lundbeck as one of several speakers. Julie will give a talk titled: Finding Na_V1.1 activators – development and validation of a HTS suitable assay on the Qube. Also Noah Shuart from Xenon will be giving a talk.

Venue:

Sophion Bioscience, Inc.
400 Trade Center Drive, Suite 6900, Woburn, MA 01801

Agenda:

April 10th

11.30 AM        Registration and lunch buffet

01.00 PM        Presentations

02.30 PM        Coffee break

03.00 PM        Presentations

04.30 PM        Wrap up

05.30 PM        Wine tasting event onsite

April 11th

08.45 AM        Registration and coffee

09.30 AM        Presentations

10.30 AM        Coffee break

12.00 Noon     Lunch

02.00 PM        Wrap-up

Local hotels:

Hilton Boston/Woburn
2 Forbes Road, Woburn, MA
Phone: +1 781-932-0999

Crowne Plaza Boston/Woburn
15 Middlesex Canal Park Drive, Woburn, MA
Phone: +1 781-935-8760

Comfort Inn Boston/Woburn
14 Hill St, Woburn, MA 01801
Phone: +1 781-933-5363

Registration for ICMS2018 is now open

Wednesday and Thursday 20th and 21st June, 2018 Sophion will be arranging and hosting the third Ion Channel Modulation Symposium at Clare College in Cambridge (UK) and it is now possible to register for the event.

Click here to read more.

We look forward to seeing you in Cambridge next June.

Santa’s little helpers…..?

No, this is not Santa Claus’ little helpers packing up toys for children, but our great production guys getting more systems ready for our happy customers.

Fast desensitizing ion channels recorded on Qube 384

Some ligand gated ion channels have a tendency to desensitize over time, making it difficult to establish a stable assay baseline. Rapid compound washout can counteract desensitization by reducing ligand exposure time to a minimum.

On Qube 384 the minimum washout is now less than 1 second (0.8 s), enabling stable assay for fast desensitizing ion channels.

With nAChRa1 as model, acetyl choline as agonist and tetracaine as test compound, a stable and high performance assay was established with:

• Ligand exposure time 0.8 s
• Whole-cell resistance of average 1.2 GΩ
• Overall success rate of 89%
• Very tight data – CV of ≤ 9% for control rows and columns
• Z’ > 0.70
• No desensitization observed

You can read the whole report here.

Five new QPatch publications from top pharma companies

The past month five new publications has been published from GSK, Pfizer, Gilead, Lundbeck and Acesion Pharma.

Donovan et Al 2017 – Discovery and electrophysiological characterization of SKF-32802: A novel hERG agonist found through a large-scale structural similarity search

Jenkinson et Al 2017- Cardiac sodium channel antagonism – Translation of preclinical in vitro assays to clinical QRS prolongation

Diness et Al 2017 – Termination of vernakalant-resistant atrial fibrillation by inhibition of small-conductance Ca²⁺-activated K⁺ channels in pigs

El-Bizri et Al 2017 – Eleclazine exhibits enhanced selectivity for long QT syndrome type 3–associated late Na⁺ current

Schoubye et Al 2017 – The sodium channel activator Lu AE98134 normalizes the altered firing properties of fast spiking interneurons in Dlx5/6^+/− mice

Sophion user meeting in our new facilities in Japan

To accommodate the needs of a growing customer base in Japan, we have expanded our laboratory and demo space in our Japanese facilities in Honjo-Waseda. This was celebrated with a three day user meeting; two days with work shop and one day with seminar with great talks on science. Both the demo room with QPatch and Qube side by side as well as the conference room were in use to accommodate the approx. 30 users that wanted to learn about the latest tips, tricks and software for QPatch and Qube 384. A great success with active interaction and continuing into the evenings with delicious Japanese foods.

High throughput screening for mode-of-action on Nav1.4

A high-fidelity patch clamp set up is necessary to discover use-dependent mode of action. Qube is a second generation automated patch clamp system that fulfills this requirement and allows for testing of many thousands of compounds per day in an unattended fashion. Using Qube in a drug development cascade allows to ask the right questions during the primary screen, making a follow-up validation study obsolete. Some key points for a Qube screening like this are:

• Giga-ohm seal
• 99% average success rates
• Very tight data
• Discrimination between different modes-of-action

To read the full report click here

ICMS 2018

The dates have been fixed so mark your calendar for the 20th and 21st June, 2018. We look forward to seeing you at Clare College in Cambridge next year.

More information will be posted here shortly.

ICMS 2018

We are thrilled to announce the dates for next years’ Sophion Ion Channel Modulation Symposium and look forward to seeing so many ion channel professionals again next June.

The venue is the same as the previous two years: Clare College in Cambridge and the dates are 20th and 21st June, 2018.

See much more information about this meeting here.

Biophysical Society 62nd Annual Meeting

We look forward to Biophysics 2018 where we will be doing a lot of activities:

First of all you can meet with our ion channel experts at our booth #518 at the Moscone Center.

Satellite Meeting

Friday, 16th February Sophion will be hosting the annually recurring satellite meeting, Drug Discovery for Ion Channels. 

See the agenda for the meeting here and make sure to sign up as the spaces are limited. 

Beer Tasting & Dinner

Saturday, 17th February we have the pleasure of inviting you to an informal evening of beer tasting, good food and great networking at the Bartlett Hall in San Francisco.

Make sure to sign up for this event here. Limited number of seats so be quick.

Ion Channel Mini Symposium

Tuesday, 20th February we will be having a short meeting at the conference center with the presentation title: Drug discovery and electrophysiological characterization using automated patch clamp (QPatch).

Venue: Room 6, Moscone Center, San Francisco – sign up here for the meeting:

10:30 – 11:00
Dr Damian Bell, Iontas Ltd.
Efficient ion channel cell line generation using MaxCyte electroporation and QPatch validation

11:00 – 11:30
Dr Daniel Sauter, Application Scientist, Sophion Bioscience A/S
Induced pluripotent stem cell-derived cardiomyocytes (Cor.4U) characterized on an automated planar patch clamp set up (QPatch HT)

11:30 – 12:00
Dr Alan Wickenden, Scientific Director & Fellow, Molecular & Cellular Pharmacology, Janssen R&D, L.L.C
NaViGATING the long and winding road to new analgesics: Discovery of potent, selective, closed-state peptide Nav1.7 blockers

Refreshments will be served.

Poster Presentation

Wednesday, 21st February between 10.30 AM and 11.30 AM, Dr Daniel Sauter will present a poster titled:

Induced pluripotent stem cell-derived cardiomyocytes (Cor.4U) characterized on an automated planar patch clamp setup (QPatch HT)

Poster board no. B301

Eight new QPatch publications, two of them in Nature.com

A lot of new peer reviewed publications have seen the light over the summer. Here is some selected new publications. For more interesting publilcations on QPatch and Qube you can always search our publication database here

Huang et Al 2017 Synthesis and biological evaluation of novel 6,11-dihydro-5H-benzo[e]pyrimido- [5,4-b][1,4]diazepine derivatives as potential c-Met inhibitors

Kristof et Al 2017 An Official American Thoracic Society Workshop Report: Translational Research in Rare Respiratory Diseases. Official workshop report of the American Thoracic Society

Lazewska et Al 2017 Biphenyloxy-alkyl-piperidine and azepane derivatives as histamine H3 receptor ligands

Menegon et Al 2017 A new electro-optical approach for conductance measurement: an assay for the study of drugs acting on ligand-gated ion channels

Prashanth et Al 2017 Pharmacological screening technologies for venom peptide discovery

Sousa et Al 2017 Discovery and mode of action of a novel analgesic β-toxin from the African spider Ceratogyrus darlingi

Zhou et Al 2017 Design, synthesis and biological evaluation of 4,7,12,12a-tetrahydro-5Hthieno [3′,2’:3,4]pyrido[1,2-b]isoquinolines as novel adenosine 5′-monophosphate-activated protein kinase (AMPK) indirect activators for the treatment of type 2 diabetes

Zidar et Al 2017 Clathrodin, hymenidin and oroidin, and their synthetic analogues as inhibitors of the voltage-gated potassium channels

Poster presented at SPS in Berlin in September on temperature effect using Qube

Until recently, the only possibility to test compound potency under voltage control conditions has been the manual patch clamp technique. Now automated patch clamp instruments with temperature control have become available making it possible to perform up to 384 parallel recordings at controlled temperatures ranging from 8°C and above. Qube has a temperature controlled test environment and in these studies, we show that temperature merits being taken into consideration when evaluating for hERG pharmacology. See the poster here.

New faces at Sophion

To meet the increasing demand of new application development and customer support, we have hired two new application specialists.

Kim Boddum has a PhD in neuropharmacology and comes from a post doc at the Department of Biomedical Sciences at the Uni of CPH. Kim has for the past 7-8 years worked on membrane receptors and ion channels function and pharmacology.

Kadla Røskva Rosholm has a PhD in Nanoscience working on high-throughput fluorescence-based cell assays. Also she been done two post docs working on electrophysiological and fluorescence methodologies to investigate the molecular mechanism of ion-channel signaling.

You can meet Dr. Kadla Røskva Rosholm and Dr. Kim Boddum at customer sites, demos or conferences.

Qube 384 recordings with very short exposure time of ligand

Some like it slow, some like it fast. A Qube user wanted faster washout of activator in ligand-gated experiments and contacted their application scientist. We adapted the protocol in a matter of a week to obtain faster washout of ligand. That is how versatile the Qube Viewpoint software is. We thus reduced the ligand exposure time from 32 s to 0.8 s. The user has already used it and presented data on our Sophion User Meeting last week in Paris. Above is shown data from applying EC₂₀ concentration of Acetylcholine to AChRa1 with the slow protocol (32 s) respectively the fast (0.8 s) protocol. There was not used esterases in any of the washouts. With the fast protocol it is clear that the current can be stimulated multiple times without desensitization.

Sophion Seminar & Workshop – Japan

You are invited to the Sophion Seminar & Workshop in Japan at Sophion Bioscience K.K.’s premises:

Venue

Waseda Research Park
1011 Nishitomida, Honjo, Saitama 367-0035, Japan

Programme

10:00          Registration

10:30          Welcome remarks and safety briefing
Dr. Yuji Tsurubuchi, Country Manager, Sophion Bioscience K.K., Japan

10:40          New ownership and future strategy at Sophion (tentative)
Mr. Thais Johansen, CEO, Sophion Bioscience A/S, Denmark

11:00          Educational lecture: Redox Physiology of TRP channels
Prof. Yasuo Mori, Laboratory of Molecular Biology, Department of Synthetic Chemistry and Biological Chemistry, Graduate School of Engineering, Kyoto University, Japan

12:00          Lunch break and new Sophion K.K. lab tour
Each participant is assigned to either group A or B at the time of registration. The tour starts at 12:00 and 12:45 for group A and B, respectively. Lunch is served for group A after the tour.

13:30          Potency of ReproNeuro “Human iPS derived neurons” in the drug discovery support
Dr. Makoto Honda, ReproCELL, Inc., Japan

13:50          iPS derived human cells; iCel®, MyCell® DDP/ “disease in a dish” and ideas of application for drug discovery
Dr. Ko Zushida, Cellular Dynamics International Japan Co., Ltd.

14:20          Using the QPatch HTX to drive drug discovery: ligand-gated ion channels
Dr. Robert E. Petroski, Scientist IV/Manager Neurophysiology, Dart Neuroscience LLC, USA

15:00          Coffee break

15:30          Targeting T-type calcium channel for anti-pain drug discovery
Dr. Norio Hashimoto, Nissan Chemical Industries, Ltd., Japan

16:10          Exemplar of optical recording from neural and cardiac activities
Mr. Kenji Tsubokura, Brain Vision Co., Ltd., Japan

16:30          CiPA – novel drug safety assessment
Ms. Melanie Schupp, Application Scientist, Sophion Bioscience A/S, Denmark

16:50          Closing remarks
Mr. Naoto Ueda, President & CEO, Physio-Tech Co., Ltd., Japan

16.55          Bus transportation to the venue of reception

17:30          Reception (food and beverages are served)
Saitama Grand Hotel Honjo

19:30          Bus transportation to Honjo Waseda Station

Tecan publishing article about QPatch

We are proud to share with you an article published in Tecans latest journal about Sophion and our work with the QPatch. You can read the article here.

See some of the great talks from ICMS 2017 in Cambridge

We have the pleasure of sharing with you some of the great talks from the Sophion Ion Channel Modulation Symposium which took place in Cambridge in June.

See the talks here.

Enjoy

Qube version “Duck” is now available

Enjoy current clamp combined with voltage clamp in the same sweep and on all 384 sites to make you results very tight. Cool or heat at the recording site to investigate the temperature sensitivity of the pharmacology you are interested in. Load Qube with stock solutions and let it dilute it to the final test concentration only seconds before adding it to the cell. This and many more updates is the latest results of the constant development Sophion is putting into our products based on inputs from our customers.

Temperature control on Qube 384 – pharmacological dependency of hERG reference compounds

Studies of temperature dependencies can be done efficiently and reliably on Qube 384. In this study we directly measure change in potency with change in temperature on four different compounds, emphasizing the importance of temperature when studying drug candidates.

See the new application report here.

Sophion Bioscience is acquired by Sophion CEO, management and investors

Sophion Bioscience has been acquired by Sophion CEO Thais T. Johansen, its management and a group of experienced investors.

Sophion was founded in 2000 as a spinoff from Neurosearch and have since the beginning been pioneering ion channel research and drug discovery. In 2004 Sophion launched the QPatch automated patch clamp solution, which still today is benchmark for advanced electrophysiology and cardiac safety in drug discovery. In 2013 Sophion Qube was launched taking automated patch clamp to the HTS space and taking automated patch clamping to a whole new level of usability. In between Sophion has continuously improved performance and capabilities and launched pioneering new features such as automated Rs compensation, automated current clamp, integrated cell preparation, etc.

Sophion was in 2011 acquired by Biolin Scientific Holding AB, a company owned by Swedish private equity firm Ratos AB.

Sophion CEO Thais Johansen states “Our new ownership structure and financial partners bring a long-term orientation and expertise in building a high-growth life science business. With this involvement, we are well-positioned to continue investing in innovation, technologies and people”.

Thais also said, “we will continue to build on the Sophion legacy with focus on quality, innovation and customer satisfaction” and continues “I am looking forward to talk to our partners over the next weeks to discuss these changes as well as discuss the many great news we have in pipeline”.

Sophion Bioscience employs approximately 60 people worldwide. It is headquartered in Copenhagen, Denmark and has subsidiaries in Boston, Tokyo and Shanghai, as well as distributors in Japan, India and Korea. Sophion has an install base of 100+ automated patch clamp systems and presence in more than 75% of the TOP20 largest Pharma companies in the world.

Sophion Bioscience, Inc. is in the building

ICMS2017 – thanks everyone for contributing

Another great Sophion Ion Channel Modulation Symposium meeting at the amazing Clare College. Knowledge sharing, socializing and presentations of new discoveries in our field from the top notch researchers from academia and pharma industry. …. and good food and beer not to mention. Great way to spend a week. ICMS2018 already in pipeline.

Ph.D. course at Sophion Denmark

Sophion was hosting a PhD summer school on cardiac electrophysiology Wednesday the 7th of June.
The course consists of 30 students from many different institutions all around Europe and will be in conjunction with a European Marie Sklodowska Curie training network.
The students will be introduced to our company and the spirit of Sophion Bioscience but will also learn about patch clamp technique and even get some hands-on experience with our high throughput devices.

New paper on KCa2.X (SK) on QPatch

Small conductance calcium-activated K+ channels (KCa2.X, SK channels) are promising new targets for the treatment of Atrial fibrillation (AF), the most common type of arrhythmia. In a collaboration with Acesion Pharma, Bo Bentzen and his group revealed an inhibitory effect of some established AF drugs on SK channels using Sophion`s QPatch.   The paper benefits from QPatch`s capability to gain gigaohm seal resistances without relying on the presence of seal enhancing fluoride in the internal solution.

Read more here

Interested in CFTR? ….or traditional Chinese/Japanese medicine?

Another paper has just been published using QPatch, showing that the Kampo medicine Mashiningan (MNG) improves opioid-induced constipation in rats by activating cystic fibrosis transmembrane conductance regulator. The effects were determined using QPatch.

To our knowledge this is one of the first papers on traditional Japanese/Chinese medicine-based on studies with a QPatch, which we find rather exciting.

For those of you who are not acquainted with Japanese Kampo, it is based on traditional Chinese medicine but adapted to Japanese culture. Kampo is widely practiced in Japan, and is fully integrated into the modern healthcare system.

You can read more about Kampo here and read more from the paper here

Ion channel blocking antibodies

Exciting work from Iontas. Concentration-dependent inhibition of Kv1.3 and ASIC1a currents were demonstrated using QPatch automated patch clamp.

Read more here

Internal solution exchange on Qube 384 – New application report

Internal addition of compounds targeting the chloride channel CIC-1.

We demonstrate a robust ClC-1 assay on Qube with internal addition of compounds. The assay shows biophysical characteristics as expected for ClC-1 with good pharmacology and high Z-score. We further introduce Sophion`s Analyzer software that allows rapid analysis of large data sets to answer advanced electrophysiological questions, in the present case: What is the mode of action of a novel, unknown compound?

See the full application report here

Sophion in the US is moving to Boston

We are happy to announce that we will be moving our US facilities to Boston over the summer. The Boston offices and laboratory will, when finished, be fully operational for application and assay development, and as a training and demonstration laboratory for customers and development partners. Although our current laboratory in New Jersey was conveniently close to Manhattan and the Yankee Stadium, we have for the last couple of years wanted to move to Boston. The recent split from Biolin Scientific gave us that opening. Keep the line open and wait for the invitation for housewarming during the autumn.

New Nature paper on QPatch and neuronal stem cells

A group from University of Rostock has together with Sophion proved the feasibility of automated electrophysiological characterization of neuronal cells. The automated electrophysiology was done on a Sophion QPatch. With the QPatch’ unique ability to create gigaseals in physiological solutions the QPatch has again has shown its worth for advanced ephys measurements.

The QPatch data was done during a 6 weeks stay at Sophion as a part of Denise Franz Pd.D project. Congrats on the publication Denise, hope to see you again soon.

Read more here

Sophion User Meeting – Paris

We are happy to invite you to our European Sophion User Meeting on 7th and 8th September and we are very pleased to announce that Sanofi in Paris kindly has offered to host the meeting this year.

We are preparing an interesting programme starting at noon on 7th September giving everyone a chance to travel to Paris in the morning. Wrap-up on 8th September just around lunchtime.

À bientôt

Sponsors:

Safety Pharmacology Society annual meeting

Hope to see you at the annual Safety Pharmacology Meeting 2017 in Berlin. Meet us at booth #113 and speak with our ion channel experts on site.

When:  24th to 27th September

Venue: Maritim Hotel Berlin

Poster presentation (Poster #022)
Temperature effect on hERG channel pharmacology measured by using the Qube automated patch clamp system.

Abstract:

The human ether-à-go-go related gene (hERG) function is important for cardiac repolarization and inhibition of the channel can prolong the cardiac action potential, which give increased risk for ventricular arrhythmias including torsade des points (TdP). Therefore, In vitro evaluations of the compound effects is performed on the hERG channel routinely in drug development projects to detect potential arrhythmic side-effects.

Usually these compound measurements are carried out at ambient temperatures. Previously it has been shown that the potency for many compounds have been underestimated when compared to near physiological temperature tests. Therefore, a temperature controlled measuring environment is beneficial when testing compounds for the aims as mentioned here.

Until recently, the only possibility to test compound potency under voltage control conditions has been the manual patch clamp technique. Now automated patch clamp instruments with temperature control have come available making it possible to perform up to 384 parallel recordings at controlled temperatures ranging from 18°C and above.

Here we used an automated patch clamp system, Qube, to study the effect of temperature on concentration response relationships on a panel of compounds known to block the hERG channel. Qube has a temperature controlled test environment and in these studies, we show that temperature merits being taken into consideration when evaluating for hERG potency.

Neuroscience

See you at Neuroscience 2017, the world’s largest neuroscience conference for scientists and physicians devoted to understanding the brain and nervous system. You can find us at booth #823 where we look forward to meet you for an ion channel talk.

Venue:  Walter E. Washington Convention Center, Washington, DC

Ion Channel Modulation Symposium 2017 – see the agenda

We are working with the final details for this years’ agenda and we are very proud of the line up. Again this year we have a good programme with excellent speakers and interesting topics.

You can see the agenda here.

Voltage- and current clamp on induced pluripotent cardiomyocytes with Qube 384

Action potentials are induced in both HL-1 mouse atrial cardiomyocytes and Axiogenesis Cor.4U iPS cell-derived cardiomyocytes.

Voltage- and current clamp on induced pluripotent cardiomyocytes with Qube 384. Action potentials are induced in both HL-1 mouse atrial cardiomyocytes and Axiogenesis Cor.4U iPS cell-derived cardiomyocytes. Qube can combine voltage clamp and current clamp in the same sweep for added experimental control. Click here to read more.

Cav1.2 on Qube 384

For a long time, screening assays on Ca_V1.2 have been challenged by the tendency of Ca_V1.2 cell lines to exhibit declining current levels in the course of the experiment. Here we report a robust assay with high success rates and reliable pharmacology.

• Success rates of 91% for Ca2+ currents and 98% for Ba2+ were achieved
• Stable currents with as low as 0.6 ± 1.8% rundown per minute
• Reference pharmacology in accordance with literature values
• Use-dependent and use-independent mode of action distinguished with different voltage protocols

The voltage-sensitive L-type Ca²⁺-channel (LTCC) Ca_V1.2 is a crucial component for controlling intracellular activity and thereby essential in the cardiovascular and neuronal system. It is widely expressed in vascular smooth muscle tissue and the heart muscle 1-3. The opening of the channels leads to an increase of intracellular calcium, which act as second messenger, and thereby affects a variety of cellular processes 4 including heart muscle contraction and Ca_V1.2 is therefore an important target in e.g. safety pharmacology screening. Ca_V1.2 channels are known to require a large depolarization for their activation and once activated they display a long-lasting current flow, which typically can be blocked by low micromolar concentrations of e.g. dihydropyridines, phenylalkylamines and benzothiazepines 5,6.

In these studies, currents from HEK-hCa_V1.2 were recorded on the high-throughput platform Qube 384 in both single-hole and multi-hole mode. Success rates, IV characteristics and the pharmacological effects of three different compounds were determined.