At Intonation, we carry out in-vitro and in in-vivo pharmacologic and physicochemical property analysis of biologically active small molecules to support drug discovery projects. We feature the assessment and optimization of Structure-Pharmacological / Property-Relationships (SPR), which may be a critical step for efficacy evaluation.
Additionally, to assess compound characteristics like solubility, protein binding, permeability, stability etc. our teams prioritize different structural classes and order them not only on potency but also in reference to potential downstream absorption or metabolic liabilities.
In-vitro – Physico-chemical characterization, cell and non-cell-based absorption, metabolism (microsomes/hepatocytes), CYP isozymes.
In-vitro ADME Screening:
Aqueous Solubility: Kinetic, Thermodynamic, Thermodynamic equilibrium solubility in water, organic solvents, buffers, formulations solvents.
Metabolic Stability: Rat, mouse, dog, human microsomes, Cryopreserved hepatocytes
Drug-drug interaction: CYP450 inhibition or CYP450 induction
Distribution: Plasma protein binding, Blood partitioning, PAMPA/Caco-2 permeation studies
Plasma stability and Plasma Protein binding: (Mouse, Rat, Dog and Human), Stability in SGF and SIF
CYP Inhibition (1A2, 2C8, 2C9, 2C19, 2D6, 3A4): both % inhibition and IC50, Time-dependent CYP inhibition
In-life Pharmacokinetics – Bioavailability, blood-brain barrier, cerebrospinal fluid, tissue distribution, etc. in rodents. Our In-vivo services include exploratory PK, PD and TK studies. Understanding the bioavailability, exposure, half-life, clearance and metabolism of a drug may be the difference between success and failure in the clinic. We provide in vivo dosing and sampling in rodents, PK bioanalysis, and report preparation.
Bioanalytical Lab Services:
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