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class="hero__content"> <h1>Fast turnaround early ADME in vitro screening available!</h1> <p class="hero__date">Posted on June 13, 2024</p> </div> </div> </div> <main class="wp-block-group main main--page is-layout-flow wp-block-group-is-layout-flow"><div class="entry-content main__content wp-block-post-content is-layout-flow wp-block-post-content-is-layout-flow"> <p>For our customers with small molecules in the hit-to-lead stage of the project, <a href="https://admescope.com/" target="_blank" rel="noreferrer noopener">Admescope</a> understands the importance of a rapid design-make-test cycle; <strong>we now guarantee results within a week for frequently occurring screenings.</strong> This is one of our many R&D updates this year. Continuous <a href="https://admescope.com/services/early-adme/?utm_campaign=Admescope%20newsletter&utm_medium=email&_hsenc=p2ANqtz-94twyzcGBnRygDy2eF9BDAnftDGS4LO4qlt8VMFk6W0dC95gINTHfmKqzpry0xdpz5mpQpLr_t3TGHlUc2k-0-r-3giXasocrkvLiBzn2pZHIjLvw&_hsmi=89369857&utm_content=89369857&utm_source=hs_email" target="_blank" rel="noreferrer noopener">early in vitro ADME</a> support is available to assess initial parameters through streamlined protocols and automation, ensuring cost-effective solutions.</p> <p>To provide an initial understanding of your compounds’ ADME profiles for fast decision-making and predicting in vivo parameters, we offer the following early ADME assays as a comprehensive package:</p> <h2 class="wp-block-heading has-medium-font-size"><strong>Kinetic solubility</strong></h2> <p>A viable drug candidate must have sufficient aqueous solubility. Early identification of solubility issues allows the medicinal chemists to optimize the compounds as much as possible. Our kinetic solubility assay, conducted in PBS at pH 7.4 coupled with LC/MS/MS analysis, offers fast and accurate assessment of initial solubility with low test compound consumption. </p> <h2 class="wp-block-heading has-medium-font-size"><strong>LogD7.4</strong></h2> <figure class="wp-block-image alignleft size-large is-resized"><img fetchpriority="high" decoding="async" src="https://admescope.com/wp-content/uploads/sites/2/2023/12/PROTAC-V2-1024x684.png" alt="Admescope lab team member - Admescope is a preclinical contract research organization (CRO)" class="wp-image-4199" width="574" height="383" srcset="https://admescope.com/wp-content/uploads/sites/2/2023/12/PROTAC-V2-1024x684.png 1024w, https://admescope.com/wp-content/uploads/sites/2/2023/12/PROTAC-V2-300x200.png 300w, https://admescope.com/wp-content/uploads/sites/2/2023/12/PROTAC-V2-768x513.png 768w, https://admescope.com/wp-content/uploads/sites/2/2023/12/PROTAC-V2.png 1083w" sizes="(max-width: 574px) 100vw, 574px" /></figure> <p>It is crucial to screen for logD and to understand compounds’ lipophilicity, which affects a wide range of ADME properties, such as absorption, permeability, stability and solubility. Our logD assay, optimized for high-throughput using liquid-handling robots, and analyzed with LC/MS/MS, provides high detection sensitivity for aqueous phase and covers a wide logD range.</p> <h2 class="wp-block-heading has-medium-font-size"><strong>Metabolic stability</strong></h2> <p>Initial metabolic stability screening is typically conducted with human and rat or mouse liver microsomes. However, for certain compounds hepatocytes may be a better alternative, and stability screening can also be conducted in hepatocytes. Later, as required, soft spot metID incubations can be conducted to detect the metabolic liabilities in the structures.</p> <h2 class="wp-block-heading has-medium-font-size"><strong>Plasma protein binding</strong></h2> <p>Understanding the level of plasma protein binding is essential, as only the unbound compound can reach its target and achieve therapeutic effects. Our early ADME package includes this assay using rapid equilibrium dialysis, the gold standard for small molecules. Typically, the assay is conducted using plasma from the same species used in the metabolic stability screening.</p> <h2 class="wp-block-heading has-medium-font-size"><strong>CYP inhibition</strong></h2> <p>With the increasing prevalence of co-medications among patients, early consideration of potential drug-drug interaction risks is crucial and encouraged to be assessed also by the regulatory authorities as early as possible. Our early ADME screening package includes screening for direct CYP inhibition of the major 7 drug-metabolizing CYPs using an affordable and efficient cocktail approach. The tendency for time-dependent inhibition as IC<sub>50</sub>/IC<sub>50</sub> shift determination can also be investigated as required.</p> <figure class="wp-block-image aligncenter size-large is-resized"><img decoding="async" src="https://admescope.com/wp-content/uploads/sites/2/2024/06/007-Admescope-lab-small-picture-1024x683.png" alt="" class="wp-image-5099" width="553" height="369" srcset="https://admescope.com/wp-content/uploads/sites/2/2024/06/007-Admescope-lab-small-picture-1024x683.png 1024w, https://admescope.com/wp-content/uploads/sites/2/2024/06/007-Admescope-lab-small-picture-300x200.png 300w, https://admescope.com/wp-content/uploads/sites/2/2024/06/007-Admescope-lab-small-picture-768x512.png 768w, https://admescope.com/wp-content/uploads/sites/2/2024/06/007-Admescope-lab-small-picture.png 1198w" sizes="(max-width: 553px) 100vw, 553px" /></figure> <h2 class="wp-block-heading"><strong>Admescope can also support beyond the in vitro early ADME assays – fast TAT in vivo PK screening</strong></h2> <p>After gathering initial in vitro data, we offer <a href="https://admescope.com/services/in-vivo-dmpk/?utm_campaign=Admescope%20newsletter&utm_medium=email&_hsenc=p2ANqtz--Q60AGhp_EB_eE6_uphbkbVpTRNRHGe4JriP9XTowE4M5mZSeJDQ10H3yuaVjoBTjg24mhh47QfE-vL6VYOrkvzWTtnfS5GKy40B3mnRr5Al07gYo&_hsmi=89369857&utm_content=89369857&utm_source=hs_email" target="_blank" rel="noreferrer noopener">in vivo PK</a> profile screening in mice and rats, typically over an 8-hour period. These protocols determine oral bioavailability but can be adapted for intravenous or oral dosing as preferred. To minimize animal use, multiple compounds can be pooled and administered as a cassette. We also provide full PK profiling, including excreta collection and rodent mass balance studies with radiolabeled compounds.</p> <p>This comprehensive suite of services ensures that our customers can efficiently advance their drug development projects with robust ADME support.</p> <p><a href="https://admescope.com/contact-us/?utm_campaign=Admescope%20newsletter&utm_medium=email&_hsenc=p2ANqtz-_b5abPEOPeNtBQSzJzdgxSsffZmYQlrZDKOyD3qQFQdKH3zvk8rwfZe1moOWsPSDFkuWfJBrnMLDjhX0RpDsLl8iRpm-lAEVl43JdP4KB_dwpr2GI&_hsmi=89369857&utm_content=89369857&utm_source=hs_email" target="_blank" rel="noreferrer noopener">Reach out to our team</a> to discuss what kind of early ADME assay panel would suit best for your needs or request a quote <a href="https://admeshop.com/collections/service-packages/products/early-in-vitro-adme?utm_campaign=Admescope%20newsletter&utm_medium=email&_hsenc=p2ANqtz--iFPS9saar5k-i-3j7Nh-0NiGkW85polO9LMj62ouCWHNaOpb22uiSKFAZUOV0_jVXnCPoDwD0DMRMhA7VV8D4IqcNQx4lIyFzoP9HivOL4hO4fjc&_hsmi=89369857&utm_content=89369857&utm_source=hs_email" target="_blank" rel="noreferrer noopener">through our Admeshop</a>!</p> </div> <section class="bgimg background-image-block" style="background-image:url('https://admescope.com/wp-content/uploads/sites/2/2023/06/home-bgimg.jpg');"></section> <section class="block block"> <div class="block__content block__content--right"> <div class="block__text"> <h2>Feel free to contact us!</h2> <p><strong>Curious to know more about what can we do for you? 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src="//js-eu1.hs-scripts.com/25214463.js"></script>  </div></div> <section class="downloads__aside" id="sidebar-downloads"> <button class="downloads__label"> <span>0</span> <svg><use xlink:href="#icon-download"></use></svg> </button> <div class="downloads__content"> <button class="downloads__close" id="downloads-close"><svg xmlns:xlink="http://www.w3.org/1999/xlink"><title>Close this panel</title><use xlink:href="#icon-times"></use></svg></button> <div id="selected-files" class="downloads__files"> <h3>Files</h3> <div> <ul></ul> </div> <button style="margin-top:20px;" id="remove-all-files" type="submit" class="button">Remove all</button> </div> <form class="downloads__form form" action="https://admescope.com/wp-admin/admin-ajax.php" method="POST" id="symeresdownloads"> <p>Please, provide us your email address so that we can send you a link for downloading the requested files.</p> <div class="form__row"> <div class="form__col"> <label for="email">Email</label> <input id="email" name="email" type="email" placeholder="Email" required> </div> </div> <div class="form__row"> <div class="form__col"> <label for="agreement"> <input id="agreement" name="agreement" type="checkbox" required> <div>By downloading, I agree to the <a href='/privacy-policy/'>privacy policy</a></div> </label> </div> </div> <div class="form__row"> <div class="form__col"> <input type="text" name="downloaded_files" value="" style="opacity: 0;height: 0;overflow: hidden;"> <button type="submit" class="button button--primary">Download file(s)</button> <input type="hidden" name="action" value="symeresdownloads"> </div> </div> </form> </div> </section><script> jQuery( document ).ready(function() { jQuery(function ($) { let downloads = {}; $('body').on('click', '#downloads-close', function(){ $('.downloads__label').css('display', 'flex'); $('.downloads__content').css('display', 'none'); }); $('body').on('click', '.downloads__label', function(){ $('.downloads__label').css('display', 'none'); $('.downloads__content').css('display', 'flex'); }); $('body').on('change', 'form.downloads', function(){ let downloadsList = ''; let filenames = {}; $('input:checkbox[name=download]').each(function(){ filenames[$(this).data('filename')] = $(this).data('filetitle'); if (this.checked) { downloads[$(this).data('download')] = $(this).data('filename'); } else { if ($(this).data('download') in downloads) { delete downloads[$(this).data('download')]; } if (localStorage.getItem('downloads')) { let downloadsFromLocalStorage = JSON.parse(localStorage.getItem('downloads')); if ($(this).data('download') in downloadsFromLocalStorage) { delete downloadsFromLocalStorage[$(this).data('download')]; localStorage.setItem('downloads', JSON.stringify(downloadsFromLocalStorage)); } } } $('input[name="downloaded_files"]').val(Object.values(filenames).join(',')); }); // set filenames + titles in localStorage if (Object.keys(filenames).length) { let filenamesJson = JSON.stringify(filenames); if (localStorage.getItem('filenames')) { let currentFilenames = JSON.parse(localStorage.getItem('filenames')); filenames = { ...currentFilenames, ...filenames }; filenamesJson = JSON.stringify(filenames); } localStorage.setItem('filenames', filenamesJson); } if (Object.keys(downloads).length) { $('.downloads__aside').css('display', 'block'); let downloadsJson = JSON.stringify(downloads); if (localStorage.getItem('downloads')) { let currentDownloads = JSON.parse(localStorage.getItem('downloads')); downloads = { ...currentDownloads, ...downloads }; downloadsJson = JSON.stringify(downloads); } localStorage.setItem('downloads', downloadsJson); } else { if (!localStorage.getItem('downloads')) { localStorage.removeItem('downloads'); } } Object.keys(downloads).forEach(key => { let label = $('.downloads li label[for="download-file-' + downloads[key] + '"]').text(); if (localStorage.getItem('downloads')) { let downloadsFromLocalStorage = JSON.parse(localStorage.getItem('downloads')); if (localStorage.getItem('filenames')) { let filenames = JSON.parse(localStorage.getItem('filenames')); if (downloadsFromLocalStorage[key] in filenames) { label = filenames[downloadsFromLocalStorage[key]]; } } if (label === '') { label = $('.downloads li label[for="download-file-' + downloadsFromLocalStorage[key] + '"]').text(); } } downloadsList += '<li><button data-download="' + key + '"><svg class="downloads__delete"><use xlink:href="#icon-times"></use></svg></button><span><svg class="downloads__icon"><use xlink:href="#icon-download-file"></use></svg></span>' + label.trim() + '</li>'; }); $('.downloads__label span').text(Object.keys(downloads).length); $('#selected-files ul').html(downloadsList); // if (Object.keys(downloads).length) { //if (localStorage.getItem('downloads')) { // $('.downloads__aside').css('display', 'block'); // } else { // $('.downloads__aside').css('display', 'none'); // } }); if (localStorage.getItem('downloads')) { let downloadsFromLocalStorage = JSON.parse(localStorage.getItem('downloads')); let downloadsList = ''; $("input[name='downloaded_files']").val(Object.values(downloadsFromLocalStorage).join(',')); Object.keys(downloadsFromLocalStorage).forEach(key => { $(".downloads ul").find("[data-filename='" + downloadsFromLocalStorage[key] + "']").prop('checked', true); let label = ''; if (localStorage.getItem('filenames')) { let filenames = JSON.parse(localStorage.getItem('filenames')); if (downloadsFromLocalStorage[key] in filenames) { label = filenames[downloadsFromLocalStorage[key]]; } } if (label === '') { label = $('.downloads li label[for="download-file-' + downloadsFromLocalStorage[key] + '"]').text(); } downloadsList += '<li><button data-download="' + key + '"><svg class="downloads__delete"><use xlink:href="#icon-times"></use></svg></button><span><svg class="downloads__icon"><use xlink:href="#icon-download-file"></use></svg></span>' + label.trim() + '</li>'; }); $('.downloads__label span').text(Object.keys(downloadsFromLocalStorage).length); $('#selected-files ul').html(downloadsList); $('.downloads__aside').css('display', 'block'); } else { $('.downloads__aside').css('display', 'none'); } $('body').on('click', '#remove-all-files', function(){ localStorage.removeItem('downloads'); $('#selected-files div ul li').remove(); $('.downloads__aside').css('display', 'none'); location.reload(); }); $('body').on('click', '#selected-files button', function(){ $('form.downloads input[data-download=' + $(this).data('download') + ']').prop('checked', false).trigger('change'); if (localStorage.getItem('downloads')) { let downloadsLocalObj = JSON.parse(localStorage.getItem('downloads')); if ($(this).data('download') in downloadsLocalObj) { delete downloadsLocalObj[$(this).data('download')]; localStorage.setItem('downloads', JSON.stringify(downloadsLocalObj)); //reload sidebar html let downloadsList = ''; Object.keys(downloadsLocalObj).forEach(key => { $(".downloads ul").find("[data-filename='" + downloadsLocalObj[key] + "']").prop('checked', true); let label = ''; if (localStorage.getItem('filenames')) { let filenames = JSON.parse(localStorage.getItem('filenames')); if (downloadsLocalObj[key] in filenames) { label = filenames[downloadsLocalObj[key]]; } } if (label === '') { label = $('.downloads li label[for="download-file-' + downloadsLocalObj[key] + '"]').text(); } downloadsList += '<li><button data-download="' + key + '"><svg class="downloads__delete"><use xlink:href="#icon-times"></use></svg></button><span><svg class="downloads__icon"><use xlink:href="#icon-download-file"></use></svg></span>' + label.trim() + '</li>'; }); $('.downloads__label span').text(Object.keys(downloadsLocalObj).length); $('#selected-files ul').html(downloadsList); $('.downloads__aside').css('display', 'block'); } } }); $('#symeresdownloads').on('submit', function (e) { e.preventDefault(); if (localStorage.getItem('downloads')) { downloads = JSON.parse(localStorage.getItem('downloads')); $("input[name='downloaded_files']").val(''); $("input[name='downloaded_files']").val(Object.values(downloads).join(',')); } var symeresdownloads = $('#symeresdownloads'); var email = $("#symeresdownloads :input[name='email']").val(); var firstName = $("#symeresdownloads :input[name='first-name']").val(); var lastName = $("#symeresdownloads :input[name='last-name']").val(); var company = $("#symeresdownloads :input[name='company']").val(); var action = $("#symeresdownloads :input[name='action']").val(); downloads['email'] = email; downloads['first-name'] = firstName; downloads['last-name'] = lastName; downloads['company'] = company; downloads['action'] = action; runAjaxCall(symeresdownloads, downloads); // Clean up the downloads object delete downloads['email']; delete downloads['first-name']; delete downloads['last-name']; delete downloads['company']; delete downloads['action']; e.preventDefault(); }); function runAjaxCall(symeresdownloads, downloads) { var array = Object.keys(downloads).map((key) => [String(key), downloads[key]]); $.ajax({ url: symeresdownloads.attr('action'), data: downloads, // form data type: symeresdownloads.attr('method'), // POST beforeSend: function (xhr) { jQuery('#symeresdownloads button').hide(); jQuery('<p class="download-status">Your file(s) are being processed.</p>').insertAfter('#symeresdownloads button'); }, success: function (data) { let error = false; if (data.includes('address') || data.includes('download')) { if (!data.includes('Thank you')) { error = true; jQuery('.download-status').remove(); jQuery('.downloads__content').append('<div class="status-msg" style="font-weight:500; color: #FFF;">' + data + '</div>') } } if (data.includes('Thank you')) { error = false; jQuery('.download-status').remove(); jQuery('.downloads__content').append('<div class="status-msg" style="font-weight:500; color: #FFF;">' + data + '</div>') } setTimeout(function(){ jQuery('.status-msg').remove(); if (error) { jQuery('input#email').css('border-color', '#d63637'); location.reload(); } if (!error) { localStorage.removeItem('downloads'); $('.downloads__aside').css('display', 'none'); location.reload(); } }, 5000); } }); } if ($('.downloads__label span').text() == '0') { $('.downloads__aside').css('display', 'none'); } $('body').on('change', '.downloads__label span', function(){ if ($('.downloads__label span').text() == '0') { $('.downloads__aside').css('display', 'none'); } }); }); }); </script><script id="wp-block-template-skip-link-js-after"> ( function() { var skipLinkTarget = document.querySelector( 'main' ), sibling, skipLinkTargetID, skipLink; // Early exit if a skip-link target can't be located. if ( ! skipLinkTarget ) { return; } /* * Get the site wrapper. * The skip-link will be injected in the beginning of it. */ sibling = document.querySelector( '.wp-site-blocks' ); // Early exit if the root element was not found. if ( ! sibling ) { 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