Medicilon's Metabolite Identification Services

Metabolite identification (MetID) plays an important role in drug discovery and development process. During the lead optimization stage, early MetID study can help identify the metabolic “soft spots”, so medicinal chemists can make appropriate structure modification to improve the pharmacokinetic properties of the compounds. During the IND-enabling stage, the information obtained from cross-species metabolite profiling can guide the selection of animal species for safety assessment, which is the approach advocated by the guidance documents from regulatory agencies. In addition, reactive metabolites may trigger organ toxicity, especially hepatic toxicity. Early screening for reactive metabolite formation by GSH trapping can help minimize this risk.

Medicilon's MetID Services

Medicilon recently added Thermo Scientific Q Exactive HF-X BioPharma, one of the most advanced high resolution mass spectrometers (HRMS), into the powerful arsenal of its DMPK/BAS Division. QE HF-X is a Quadrupole-Ultra High-Field-Orbitrap mass spectrometer with a resolution up to 240,000 FWHM, high precision (< 1ppm), high sensitivity (with High Capacity Ion Transfer Tube and Electrodynamic Ion Funnel), high scan speed (up to 40 Hz), and high mass stability (without the need for frequent recalibration), outperforming the majority of commonly used HRMS. It is also complemented by Thermo Vanquish Flex UHPLC, Diode Array Detector (DAD), Variable Wavelength Detector (VWD), Compound Discoverer software, and BioPharma Finder software.

Medicilon MetID Services

Our seasoned MetID scientists utilize this high-end UHPLC-HRMS system to provide fast and reliable in vivo and in vitro metabolite identification and GSH trapping services, and have successfully completed many different types of studies from clients around world, including some challenging peptide MetID works.

List of Services (Available for Early Discovery and IND-Enabling)

In Vitro Metabolite Identification in Following Matrices

Liver microsomes

Hepatocytes

S9 Fraction

Cytosol

Plasma

Screening for Reactive Metabolites

GSH Trapping

In Vivo Metabolite Identification in Following Matrices

Plasma

Urine

Bile

Feces

Tissues and organs

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Inventory of the three major in vitro pharmacokinetic research methods

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Enzyme Activity Assay Service

Enzymatic assay Lance Assay Alphascreen Assay Z’-LYTE Assay Adapta Assay Kinase-Glo Assay ADP-Glo Assay Ligand Binding Assay ELISA Assay HTRF Assay Enzyme activity assays are laboratory methods for measuring enzymatic activity. They are vital for the study of enzyme kinetics and enzyme inhibition. Enzyme units : Amounts of enzymes can either be expressed as molar amounts, as with any other chemical, or measured in terms of activity, in enzyme units. Medicilon provides various enzyme activity assays for kinases , phosphatases, proteinases, deacetylase, peptidase, esterase, and other enzymes. Our line of well-characterized immunoassays and biochemical kits ensures accurate and reproducible results. Enzyme is a large category of bio-molecules that catalyze various biological processes including metabolic processes, cellular signaling and regulation, cell division and apoptosis. Enzymatic reactions convert substrate molecules into chemically modified molecules products with high sp

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