As a well-recognized leader in the field of drug discovery and development, plus over a decade of experience, Creative Biolabs is dedicated to the development of PROTAC®s and we offer our clients with comprehensive superior services for small molecule solubility and chemical stability.
At early stage of PROTAC® development, liquid formulation is essential to determine the cytotoxicity profile, bioavailability and pharmacokinetics, etc. Even though the superior pharmacological properties of PROTAC® candidates, they may withdraw from drug development if the aqueous solubility is poor. Hence, aqueous solubility and stability are two of the main physicochemical properties to be optimized for drug discovery. Here are potential troubles arising from poor aqueous solubility:
An ideal compound must be able to reach effective concentrations. The lowest solubility is related to its pharmacologic potency and permeability. If a compound is not solubility limited, then the drug development will be more efficient. For in vitro assays, the concentrations of up to 30 μM is needed to produce accurate results.
Aqueous solubility is one of the key factors that determine the chemical properties of a compound. Creative Biolabs provides several solubility prediction services to promote the drug development process. We provide in silico prediction to calculate the intrinsic solubility which is the concentration in equilibrium with the solid phase that dissolved into the solution. In addition, we can also predict the solubility at a given pH. Both quantitative and qualitative results can be provided, giving the solubility in logS, mol/L, mg/mL units.
Poor soluble compounds can significantly reduce productivity in drug discovery and development. Creative Biolabs provides efficient and reproducible assays to determine the aqueous solubility of small molecules, including shake flask solubility and concentration determination using HPLC-UV, liquid chromatography-tandem mass spectrometry (LC-MS) analysis, and solution calorimetry methods etc. The choice of which assay depends on the nature and applications of the PROTAC® candidate. A customized assay can be yielded according to the following four consecutive steps (see Fig.1).
Fig.1 Modular setup of assays for solubility determination.
The solubility and stability of PROTAC®s are vital when they are turned into effective drugs. Creative Biolabs offers our clients with traditional approaches to enhance the solubility including chemical modifications, physical modifications, and carrier system utilization. In addition, Creative Biolabs has established an advanced high throughput screening (HTS) platform to help our clients to identify the optimal excipients to enhance the solubility and stability of PROTAC®s with low costs and reduced timelines. With this HTS platform, we can examine the solubilization capacity of 30 various excipients, and screen the conditions in 96 well-plates.
The above assays can be customized as per the requirements of our clients, such as buffer choice, prediction method, measurement method, etc. We aim to tailor the best assay to fit your projects.
Creative Biolabs is committed to providing small molecule solubility and chemical stability services to research institutes or pharmaceutical companies to reduce the development timelines. We aim to help our clients to bring candidate drugs to be marketed faster. If you have any requirements, please just feel free to contact us right now!
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