Organochem’s Post

In vitro ADME (give rodents a break!) Are you interested in speeding up your lead optimization? So, you’ve discovered novel molecules that are potent against an exciting new biological target; now what? Will any of your molecules be able to reach the target in the context of a whole organism? To find out will certainly involve animal testing to understand in vivo pharmacokinetics and pharmacodynamics. However, testing every compound of interest in vivo is expensive and can require the sacrifice of many animals. Triaging compounds using in vitro ADME during lead optimization is more efficient and cost-effective. This approach will help your team simultaneously optimize potency and compound properties and select better compounds for in vivo studies. At GD3, we have assays for plasma protein binding, solubility, permeability, and metabolism, among others. Please speak with one of GD3’s experts to learn more about how our in vitro ADME team can advance your drug discovery and development program. Click the following link to for more information, https://lnkd.in/ezTBzjzk

In vitro ADME (give rodents a break!) Are you interested in speeding up your lead optimization? So, you’ve discovered novel molecules that are potent against an exciting new biological target; now what? Will any of your molecules be able to reach the target in the context of a whole organism? To find out will certainly involve animal testing to understand in vivo pharmacokinetics and pharmacodynamics. However, testing every compound of interest in vivo is expensive and can require the sacrifice of many animals. Triaging compounds using in vitro ADME during lead optimization is more efficient and cost-effective. This approach will help your team simultaneously optimize potency and compound properties and select better compounds for in vivo studies. At GD3, we have assays for plasma protein binding, solubility, permeability, and metabolism, among others. Please speak with one of GD3’s experts to learn more about how our in vitro ADME team can advance your drug discovery and development program. Click the following link to for more information, https://lnkd.in/ezTBzjzk

In vitro ADME (give rodents a break!) Are you interested in speeding up your lead optimization? So, you’ve discovered novel molecules that are potent against an exciting new biological target; now what? Will any of your molecules be able to reach the target in the context of a whole organism? To find out will certainly involve animal testing to understand in vivo pharmacokinetics and pharmacodynamics. However, testing every compound of interest in vivo is expensive and can require the sacrifice of many animals. Triaging compounds using in vitro ADME during lead optimization is more efficient and cost-effective. This approach will help your team simultaneously optimize potency and compound properties and select better compounds for in vivo studies. At GD3, we have assays for plasma protein binding, solubility, permeability, and metabolism, among others. Please speak with one of GD3’s experts to learn more about how our in vitro ADME team can advance your drug discovery and development program. Click the following link to for more information, https://lnkd.in/ezTBzjzk

In vitro ADME (give rodents a break!) Are you interested in speeding up your lead optimization? So, you’ve discovered novel molecules that are potent against an exciting new biological target; now what? Will any of your molecules be able to reach the target in the context of a whole organism? To find out will certainly involve animal testing to understand in vivo pharmacokinetics and pharmacodynamics. However, testing every compound of interest in vivo is expensive and can require the sacrifice of many animals. Triaging compounds using in vitro ADME during lead optimization is more efficient and cost-effective. This approach will help your team simultaneously optimize potency and compound properties and select better compounds for in vivo studies. At GD3, we have assays for plasma protein binding, solubility, permeability, and metabolism, among others. Please speak with one of GD3’s experts to learn more about how our in vitro ADME team can advance your drug discovery and development program. Click the following link to for more information, https://lnkd.in/ezTBzjzk

In vitro ADME (give rodents a break!) Are you interested in speeding up your lead optimization? So, you’ve discovered novel molecules that are potent against an exciting new biological target; now what? Will any of your molecules be able to reach the target in the context of a whole organism? To find out will certainly involve animal testing to understand in vivo pharmacokinetics and pharmacodynamics. However, testing every compound of interest in vivo is expensive and can require the sacrifice of many animals. Triaging compounds using in vitro ADME during lead optimization is more efficient and cost-effective. This approach will help your team simultaneously optimize potency and compound properties and select better compounds for in vivo studies. At GD3, we have assays for plasma protein binding, solubility, permeability, and metabolism, among others. Please speak with one of GD3’s experts to learn more about how our in vitro ADME team can advance your drug discovery and development program. Click the following link to for more information, https://lnkd.in/ezTBzjzk

In vitro ADME (give rodents a break!) Are you interested in speeding up your lead optimization? So, you’ve discovered novel molecules that are potent against an exciting new biological target; now what? Will any of your molecules be able to reach the target in the context of a whole organism? To find out will certainly involve animal testing to understand in vivo pharmacokinetics and pharmacodynamics. However, testing every compound of interest in vivo is expensive and can require the sacrifice of many animals. Triaging compounds using in vitro ADME during lead optimization is more efficient and cost-effective. This approach will help your team simultaneously optimize potency and compound properties and select better compounds for in vivo studies. At GD3, we have assays for plasma protein binding, solubility, permeability, and metabolism, among others. Please speak with one of GD3’s experts to learn more about how our in vitro ADME team can advance your drug discovery and development program. Click the following link to for more information, https://lnkd.in/ezTBzjzk

🔬 Exciting news! Our latest scientific paper, co-authored with Jana Kejíková and other esteemed colleagues, has been published in the Molecular Pharmaceutics journal! Titled "Nebulization and In Vitro Upper Airway Deposition of Liposomal Carrier Systems," this publication delves into the fascinating realm of liposomal carrier systems and their potential for pulmonary drug delivery, and is now available online! 📰 https://lnkd.in/eaex-hKv In this study, we explore the stability of liposomal systems against nebulization and investigate their potential in delivering drugs to the lungs. Our research underscores the importance of considering realistic breathing profiles. By simulating these conditions, we aim to provide a more accurate understanding of aerosol deposition in the lungs, paving the way for personalized drug delivery solutions. 🙏 A heartfelt acknowledgment to all our co-authors for their invaluable contributions to this work! #PharmaceuticalResearch #DrugDelivery #LiposomalSystems #ScientificPublication #MolecularPharmaceutics

Complimentary studies (https://lnkd.in/e-kXbYqE; https://lnkd.in/ex2SHUDk), led by Oliver Hantschel and by Shinya Oishi and Hiroshi Murakami, demonstrate the feasibility and potential of mirror-image monobodies made of D-amino acids. They developed high-affinity D-monobodies against SH2 and MCP-1, respectively, via chemical protein synthesis and library selection (using phage and yeast display in the former, and mRNA display in the latter). Notable findings include high proteolytic stability and minimal immunogenicity of D-monobodies, novel recognition modes of L-proteins by D-monobodies, and a clever use of fragment complementation to accelerate D-monobody discovery. I can imagine orally available monobody drugs as a realistic goal.

#Orange peel polar fraction containing #feruloylputrescine may alleviate diseases related to TMAO.  [ Mouse ] [ Preclinical Study ] [ Abstract ] [ 04/2024 ] NOTES: - Orange peel polar fraction #OPP effectively regulates #atherosclerosis-related markers, #TMA and #TMAO in plasma and urine, compared to the orange peel nonpolar fraction OPNP. - These inhibitory effects are independent of changes in gut microbiota composition. - The effects are attributed to the modulation of cntA/B enzyme activity and FMO3 mRNA expression in vitro. - OPP exhibits stronger inhibitory effects on TMA production than OPNP, potentially due to its higher content of feruloylputrescine, which displays the highest inhibitory activity on the cntA/B enzyme and TMA production. https://lnkd.in/ebEvXkJy

Our latest blog post features insights from Laie Abelló Tornató and Rachel Doidge on optimizing efficacy, pharmacokinetics, and pharmacodynamics analysis. They detail the preparation of animal study samples, xenograft models, and patient samples within our integrated departments. This setup allows simultaneous monitoring of signaling pathway activity and protein biomarker levels in Bioscience while evaluating compound concentrations in DMPK, providing a powerful diagnostic tool to assess therapeutic effects. 🔗 https://lnkd.in/gC7cXUQQ #DrugDiscovery #ADME #DMPK #Bioscience #Pharmacokinetics #Pharmacodynamic