Physicochemical properties | Physicochemical properties | |
Solubility (kinetic, thermodynamic) |
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Chemical stability (Buffer, Biorelevant media) |
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Thermodynamic solubility |
Permeability | Permeability | |
PAMPA assay |
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Caco-2 cells permeability |
Protein binding | Protein binding | |
Plasma (Equilibrium dialysis, Ultrafiltration) |
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Albumin, Alpha-glycoprotein (Equilibrium dialysis, Ultrafiltration) |
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Microsomal binding |
Drug metabollism | Metabolism study | |
Plasma stability |
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Microsomal stability |
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S9 stability |
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Hepatocyte stability |
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Metabolite profiling and Met ID (in vitro) |
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Metabolite profiling and Met ID (in vivo) |
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Reactive metabolite formation (GSH trapping) |
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CYP Phenotyping (CYP1A2, 2B6, 2C8, 2C9, 2C19, 2D6, 3A4/5) |
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UGT Phenotyping (UGT1A1, 1A3, 1A4, 1A6, 1A9, 2B7, 2B15) |
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Phenotyping_metabolite formation |
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Non-CYP (FMO, CES, NAT, SULT 외) |
Drug transporter | Transport study | |
ABC transport phenotyping (efflux transporters) |
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SLC transport phenotyping (uptake transporters) |
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Peptide based uptake transport phenotyping (PEPT1/2, SMVT) |
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SLC transport phenotyping in Xenopus oocytes (OATPs, OATs, OCTs, MATEs) |
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Cryopreserved hepatocytes uptake |
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Hepatic excretion by Sandwich cultured hepatocytes |
Drug-Drug interaction | Enzyme Inhibition | |
CYP Inhibition (Screening, IC50 assay) |
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CYP inhibition (Ki assay) |
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UGT Inhibition (Screening, IC50 assay) |
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UGT inhibition (Ki assay) |
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Time-Dependent Inhibition (IC50 shift assay) |
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Time-Dependent Inhibition (Ki and Kinact) |
Transporter Inhibition | |
ABC transporter inhibition (efflux transporters_accumulation) |
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ABC transporter inhibition (efflux transporters_bi-direction) |
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SLC transporter inhibition (uptake transporters) |
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Time-dependent inhibition of OATP, IC50 shift assay |
Enzyme/Transporter Induction | |
Cell viability |
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Transporter (CYPs, UGTs, Transporters) Induction |
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Enzyme activity in human hepatocytes |
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Enzyme Induction (EC50 assay) |
BCS-Biowaiver | BCS-Biowaiver | |
Solubility |
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Chemical stability |
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Caco-2 cell permeability |
Bioanalytical services | Bioanalytical service | |
Method development |
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Method validation |
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Sample analysis |
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PK analysis |
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Radiolabeled clinical ADME studies (Mass balance, Metabolite profiling & Identification) |