Monday, August 12, 2013

Free Ligands - The Calcilytic Agent NPS2143, a Calcium-Sensing Receptor Modulator

We recently synthesised a significant quantity of the calcilytic ligand NPS2143 for our research programme on G protein-coupled receptors. NPS2143 is a negative allosteric modulator of the human calcium-sensing receptor and as such an important pharmacological tool compound. Recently, we developed and published a synthesis of optically pure NPS2143 in Beilstein Journal of Organic Chemistry (Open access journal that you should check out).
Anyway, now we have come to realise that we have a lot of this compound on the shelf that we are highly unlikely to ever use. So the idea to simply give the compound away to anyone that needs some free high quality NPS2143 popped up. So here we go! If you would like 5 mg of optically pure NPS2143 and you can fulfil the requirements below we will ship it to you:
  • You are an employee at an academic institution (Associate or Full Professor)
  • You will only use the compound for non-profit academic research purposes. Please provide a brief description (will be treated confidentially)
  • You can pay the shipment costs by courier (alternatively we will ship it by regular mail)
  • You will be kind enough to cite our paper "Synthesis of the calcilytic compound NPS 2143" if you ever publish a paper were you have used it

Please email Associate Professor Daniel Sejer Pedersen at daniel.pedersen@sund.ku.dk if you are interested.

NPS2143 is by no means the only interesting compound we have sitting on the shelf and if this turns out to be a success we will definitely offer more free compounds. Let's see what happens. D!

Friday, August 09, 2013

Faking it - Elemental Analysis!

Earlier this year I was refereeing a rather good paper and had I not taken the time to inspect the experimental section I would have accepted it with minor corrections. However, whoever wrote the experimental had clearly never run an elemental analysis before and was hopeless at making them up. The numbers were simply to good and although everything else looked great I had to reject the paper due to serious misconduct/fraud. This made me think that there must be thousands of papers out there with made up elemental and HRMS analyses  as these are really simple to make up. Have a look at this web page for inspiration for realistic elemental data: http://internal.eps.hw.ac.uk/services/analytical/chn-league.htm
After this incident I always read the experimental section first and check the spectra and I really wish that my refereeing colleagues would do the same. The crap you find in the experimental section of all journals including the most prestigious ones is simply unbelievable. Even when the experimental stuff looks great it is remarkable how many procedures we are completely unable to reproduce in our lab.
Anyway, not all hustlers are equally talented as a good friend of mine pointed out yesterday when he sent me this interesting paper by Reto Dorta and co-workers: http://pubs.acs.org/doi/abs/10.1021/om4000067
My friend simply wrote check out supplementary information page 12. And so I did and this is what I found (click on image to enlarge):

Many thanks to Reto Dorta and co-workers for this excellent example of what I guess must be classified as attempted fraud since the fake elemental analysis was never added. D!