rate and efficient experimental methods. / buffer shake flask method for determining lipophilicity. The LogD value is dependent upon the temperature of the buffer and octanol. A ratio of 2:1 v/v buffer to octanol is prepared. This assay is used to determine the LogD of a test article at pH 7.4 using the shake flask method. Hydrophilic compounds (Log D < 0) typically are highly soluble but exhibit low permeability across the gastrointestinal tract or blood brain barrier. ), isoforms (CYP1A1,CYP1B1, etc) or other relevant details. Briefly, octanol (pre-saturated with buffer) is added to the test compound and sonicated. Log D (distribution co-efficient) is used as a measure of lipophilicity. Lipophilicity is a key determinant of the pharmacokinetic behavior of drugs. Microplate reader SpectraMax Plus (Molecular Devices) is used in our lab for UV-Vis measurements. The range of Log D7.4 values which can be measured using the standard Log D7.4 shake flask assay is between -1 and 5, depending on the range of aqueous concentrations measured. Log D7.4 shake flask is one of Cyprotex's in vitro ADME screening services. By clicking on ‘Send’ I agree that my data is being transferred and used by Cyprotex and the affiliated Evotec Group. Where appropriate please specify one or more species (human, rat, mouse etc. LC-MS/MS is used to quantify the samples. the traditional shake flask method is considered the gold-standard technique for determining log D 7.4, but the associated steps are not compatible with high sample throughput.4aid to the lead optimization process of drug discovery, an efficient shake flask log D 7.4 primary screen was needed that had the LogD – Shake Flask This assay is used to determine the LogD of a test article at pH 7.4 using the shake flask method. [email protected]. 1Di L and Kerns EH. Special attention was made to the most commonly reported problems in the measurement of distribution coefficients using a shake-flask method such as mixing technique, speed and time, the temperature of experiment, type of buffer and its pH as well as n-octanol/buffer phase ratio. In order to ensure the most appropriate range is used in the assay, it is useful if a predicted Log D value is provided. Journal of Molecular Screening 16(3); 348-355 4Hughes J et al., (2008) Physicochemical drug properties associated with in vivo toxicological outcomes. (2003) Profiling drug-like properties in discovery research. Use the Log D shake flask assay to determine the lipophilicity of your compound. How do I interpret the data from the Log D assay? Email: This commonly used shake flask protocol is based on the use of Millipore Multiscreen solubility filter plates or centrifugation followed by UV-Vis quantitation of dissolved compounds. If you would like to be kept informed of our latest services, new research, events and other news please tick the box below: This website is intended to assist industry participants, customers and employees to understand Cyprotex's global operations and ambitions. Drug Discovery Today 8(7); 316-323 3Wenlock MC, Potter T, Barton P, Austin RP. .woocommerce-variation-price{ display: none !important;}, In Vitro Dissolution Absorption System (IDAS), Physicochemical Properties/Dose Selection, Surgical Models for Ocular and Cardiovascular Diseases, CYP Inhibition in Human Liver Microsomes – LC-MS/MS, Either a minimum of 300 µL of test article at 10 mM in DMSO, or 5 mg of powder, Exact molecular mass of test article and its salt form. The Evotec Group currently consists of the following companies. After separation, compound is quantified in the aqueous phase and octanol phase by LC-MS/MS and the following equation is used to calculate the Log D7.4. Log D 7.4 shake flask is one of Cyprotex's in vitro ADME screening services.
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