Emulate, Inc.’s Post

In a recent publication, Merck researchers discovered the importance of incorporating flow into preclinical in vitro models. When comparing intestinal permeability of oral peptides, conventional 2D static cultures displayed a 4000-fold increase in permeability, whereas the microfluidic Gut-on-a-Chip model displayed a 20-fold increase, which is in line with ex vivo and in vivo preclinical models: https://hubs.ly/Q02H5VH90

I am happy to share our recent work on a novel model for in vitro #cocrystal dissolution, where we try to describe and predict the drug concentration profiles resulting from the #dissolution-#supersaturation-#precipitation (DSP) behavior of cocrystals by employing a population balance-based approach. For more details, please check out the full article on #molecularpharmaceutics: https://lnkd.in/gBnNrake

Source: Talanta This study presents a new methodology combining differential mobility spectrometry (DMS) with liquid chromatography-tandem mass spectrometry (LC-MS/MS) to overcome challenges in quantifying limaprost. The method achieves high sensitivity and selectivity, making it suitable for pharmacokinetic and bioequivalence investigations. The integration of DMS with LC-MS/MS is shown to be effective in analyzing biological samples with multiple interferences.

Check out our new publication in assessing Gut-on-a-Chip model using model peptides and permeation enhancers!

If you're looking for improved ways to characterize your lipid nanoparticles (LNPs), join me for a webinar on analytical ultracentrifugation (AUC) and how it can help analyze several of your CQAs in a single experiment. The webinar will also examine AUC's ability to characterize RNA. It can determine purity and oligomerization states and whether multiple folding states are present, which could affect its stability and function.

Here’s another gem from Derek Lowe's "In the Pipeline" series. An imagined 1990s dialogue between a Section Head and a Bench Chemist in med-chem captures how revolutionary bifunctional molecules for protein degradation might have seemed. First validated in 2001 and boosted by 2012 VHL ligand discoveries, this concept faced skepticism and challenges. Fast forward, bifunctional protein degraders entered clinical trials in 2019, and now, over 18 targeted degraders, including PROTACs and molecular glues, are being tested. Article: https://lnkd.in/gBamMpQ7 #DrugDevelopment #ProteinDegradation #ClinicalTrials

Anyone working with lipid nanoparticles? Would you like to know more about your sedimentation and diffusion coefficient distributions of the LNPs, as well as the lipid and RNA components and fill rates? Register to learn what analytical ultracentrifugation can do for you.

Fully functionalized probes are designed to speed up and simplify the early stages of drug development. The introduction of the diazirine photocrosslinking moiety along with the presence of a functional acetylene group allows the screening of compounds directly in cells. In recent work, Offensperger et al. used a chemical proteomics approach to map protein-ligand interactions across the human proteome. With a library of around 400 small-molecule fragments from #Enamine ’s catalog (harboring a diazirine moiety for photocrosslinking and an alkyne functionality for click reaction and enrichment), authors integrated machine learning to predict interactions within biological systems (https://lnkd.in/dd9Tvs8T). Enamine currently has almost 8 000 fully functionalized compounds in stock and more than 1 million molecules in REAL Database. The most diverse compounds have been selected and sorted out into a small library, which has been pre-plated for the most convenient and fast delivery to our clients. For more details about Enamine Fully Functionalized Probe Library https://lnkd.in/dkwpPsij

ESTIV news: James McKim will be presenting new methodologies for drug discovery and safety using his MPS platform.   Check out his poster, "A Novel Meso-Scale MPS Integrated Organ Platform to Evaluate Usnic Acid Kinetics, Organ Distribution, and Cytotoxicity: A Case Study."   Don't miss session 3b on Tuesday, June 4th at 11am, where Jim and Kaushal Joshi will present their research on "A Pilot Study to Evaluate the Kinetics, Metabolism, and Toxicity of Coumarin in an In Vitro Three-Organ Integrated MPS Model."   See you there!   #ESTIV2024 #LifeSciences #NAMs #MPSmodel

Another unique feature of the Agilent JetStream ESI source……microdroplet antibody characterization all in a matter of micro seconds and all taking place inside the ion source.