Based on our state-of-the-art research, CD Formulation seeks to develop drugs through ADME studies. We are able to offer a wide range of in vitro ADME services and provide unrivaled experience and expertise in each area. Our company is a trusted partner and offers innovative research techniques.
ADME is the abbreviation for Absorption, Distribution, Metabolism and Excretion. The ADME properties of a drug are determined by its structure, and the determination of ADME properties of a drug can provide an important reference value for the prediction of its bioavailability and bioactivity (i.e., whether a drug can reach its target and produce corresponding therapeutic effects). As the potency of compounds increases during lead compounding and lead compound optimization, in vitro ADME assays provide the necessary data to gain insight into key physicochemical properties and structural motifs to ensure compound efficacy and safety.
Fig.1 Introduction to in vitro ADME assays. (CD Formulation)
In recent years, our in vitro ADME research team has made progress on multiple fronts. A variety of advanced ultra-high throughput LC-MS/MS analytical techniques have been utilized in in vitro ADME studies, further improving the speed, quality and throughput of the tests.
Measuring the in vitro ADME properties of nucleic acid drugs can provide significant value in predicting their bioavailability and biological activity. With the support of our comprehensive in vitro ADME services platform, you can focus on optimizing your compounds and move to the next stage efficiently and confidently.
Our in vitro ADME Capabilities
Our in vitro services provide the data-driven support you need to design, select, and advance your compounds from discovery to achieving IND milestones. Whether you need early development testing (metabolic stability, kinetic and thermodynamic solubility, plasma protein binding, etc.) or a fully integrated program, our experts will work with your team to understand your program's needs and help you move toward success.
In order to ensure the accuracy and reliability of our customers' experimental data, the standard experimental system for in vitro ADME has been validated:
Fig.2 Flow chart of in vitro ADME analysis. (CD Formulation)
Technology: Analysis of nucleic acid activity by fluorescence spectroscopy, CD spectroscopic technology
Journal: European journal of medicinal chemistry
IF: 6.0
Published: 2020
Results:
The authors synthesized novel imidazoline-benzimidazole derivatives containing differently substituted phenoxy groups with the aim of evaluating their antitrypanosomal activity, DNA/RNA binding affinity, and in vitro ADME properties. The presence of diethylaminoethylidene substituents in 18a-18c enhanced the antitrypanosomal efficacy of the derivatives, especially those containing unsubstituted and methoxy-substituted phenoxy groups, and 18a and 18c were found to be more than twice as potent as nitrofurantimos against Trypanosoma africana. It was found that they were more than twice as potent as nifurtimox against Trypanosoma africana. Fluorescence spectroscopy, CD spectroscopy, thermal denaturation assays and computational analyses showed that 18a-18c had a preference for AT-rich DNA and a pattern of binding to the secondary groove. Replacement of amidine groups with basic and less ionizable nitrogen-containing molecules failed to improve the membrane permeability of the studied compounds. Due to their structural diversity, these compounds display a range of physicochemical characteristics leading to different in vitro ADME properties, leaving room for further optimization of the biosignatures.
Fig. 3 Metabolic stability analysis in determination of MDCKII-hMDR1. (Popov A B, et al., 2020)
CD Formulation has separate teams focusing on in vitro ADME experiments and analysis, with first-class experimental and analytical capabilities and project throughput to ensure rapid and high-quality delivery, helping you to complete ADME and pharmacokinetic testing services. If you have any questions, please contact our staff and we will be at your service as soon as possible.
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