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PolyUGTs kit instructions
PolyUGTs Kit Instructions
PolyUGT metabolite kits are very easy to use. Detailed instructions and tips on how to use the kits are provided below. A detailed safety data sheet for all PolyUGT products is also available for download.
Please contact us at support@hyphadiscovery.com if you have any questions or need any advice.
PolyUGTs Screening Kit
Kit contains 11 purified PolyUGT enzymes, UDPGA, formulant (only use if needed) and a control compound.
PolyUGTs Scale-up Kit
Resupply of hit isoforms in vials at x20 volume used in the screening reaction. Multiple scale-up vials can be ordered.
PolyUGTs incubation conditions
PolyUGT reactions can be successfully performed using a range of reaction conditions but are best conducted at 27°C. Examples of suitable shakers are given in the instructions but only gentle shaking is needed. You can download this handy shaker speed calculator for determining the best rpm to use for your shaker for PolyUGTS reactions, applicable for shakers with throws of 1cm or higher. You will need to know the orbit of your shaker in cm in order to use the calculator. The calculator works for most types of shakers but please contact us for advice if your shaker has a very low orbit. Please note this calculator is different to that used for PolyCYPs incubations.
The Eppendorf Thermomixer and similar vibrational shakers (orbit of 3 mm) can be used for PolyUGTs screening kits. For these shakers we recommend using the minimum speed possible, or interval shaking, when using the 24-well block supplied with the screening kits.
For scale up reactions, please refer to the specific instructions in the link above.
Recommendations and tips
For convenience, use the 24-well square well blocks provided. Sufficient material is included to conduct one reaction per enzyme at 0.5ml volume, or to run two reactions at 0.25ml at different pHs. This is useful if formation of an acyl glucuronide is suspected, since these metabolites can be more stable at a lower pH.
Resources
Explore our library of resources comprising brochures, case studies, posters and publications about the work we do.
Introducing oxygen into a drug candidate late in the optimisation process has several applications including exploration of SAR (structure-activity relationships) and the ability to access derivatives that may possess superior properties such as improved metabolic stability and LLE (ligand-lipophilicity efficiency). Biocatalysis can provide access to chemical space in a complementary manner to chemical synthesis and provide a “one-experiment” solution to accessing multiple derivatives in parallel. This poster illustrates the application of a new biocatalysis kit, PolyCYPs®, to enable parallel synthesis of hydroxylated derivatives of drugs.
In this case study at least 2 mg of a monohydroxylated metabolite (M4), originally observed in rat liver microsomes, was required by a US pharma company. Using PolyCYPs, the target metabolite was supplied to the client together with a Certificate of Analysis within 22 days from receipt of order, exemplifying the short timelines achievable using PolyCYPs to access CYP-derived metabolites.
Hypha’s PolyCYPs kits are in routine use by pharma and agchem companies for producing human and other mammalian metabolites. One application involves use of PolyCYPs for creating radiolabelled metabolites for direct comparison with the radio profiles from mass balance and distribution study samples, necessary for regulatory filing. PolyCYPs provides a clean route for scalable access to more of the CYP-derived metabolites observed in these matrices, for definitive MetID and any tox studies deemed necessary. This is especially useful where low concentrations or unstable metabolites in the mass balance sample make structural identification difficult.
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Hypha Discovery is a UK-based CRO supporting pharmaceutical and agrochemical companies worldwide through the production of metabolites and new derivatives of drugs and agrochemicals in discovery and development.