Even though vast majority of our services are tailored according to customer’s needs, we have also fixed content&price services. These can be used as such or they can form a discussion starting point when designing a tailored study.  Products below can be modified for example by increasing or decreasing timepoints, concentrations, replicates, level of quantification, etc.

PhysChem StarterKit

Simple set of studies to reveal the aqueous solubility, Log D and pKa of NCEs. Minimal amount of a compound is needed. Used for hit molecule characterisation and to aid lead optimisation.

OptiSolv, LogD1to10, pKaDay, BindingPack, ChemStab
Dedicated studies for finding out properties of compounds. OptiSolv to study water solubility and optimal organic solvent; LogD1to10 to measure LogD from pH 1 to 10 in increments of one and including 6.5 and 7.4; pKaDay to measure pKa for about 25 compounds; BindingPack to study protein binding in up to eight species; and ChemStab to study chemical stability and identify degradation products.

Solubility 100, pKa 100 and LogD 100
Early-ADME physchem studies for 100 compounds to investigate aqueous solubility up to 1 mg/ml, pKa from 2.7 to 10.1 pH-units, and LogD between -3 and 3. Naturally, any other number of compounds can be studied as well.

MetaboPilot
Quick and easy-to-order study to find out metabolic stability and main biotransformations of NCE in human. All phase I and II metabolism pathways are enabled.

MetStab
Straightforward study to characterize metabolic stability of NCEs and to calculate enzyme kinetic values for intrinsic clearance and in vivo prediction. Used for hit molecule characterisation, lead molecule selection and to aid lead optimisation.

MetabolD (includes MetStab)
Comprehensive study to find out detailed human in vitro metabolite profile of NCE. Metabolic stability of NCE and enzyme kinetic values for in vivo prediction is included. Used for drug candidate characterisation, lead molecule selection and to aid lead optimization.

MetaboPilot, MetStab and MetaboID can be done in multiple species to be able to compare metabolic characteristics in human and different animal species. Can be used for selection of toxicology animal models. Available animal species include mouse, rat, guinea pig, rabbit, dog, monkey and minipig.

HepatoPlate
Comprehensive metabolism and drug interaction study on fresh or cryopreserved, human or animal hepatocytes in 24-well plate format. Information content includes metabolic stability, metabolite identification, accumulation of parent and metabolites to hepatocyte cells, inhibition and induction

CacoPilot
Quick and cost-effective study to get the first idea of Caco-2 permeation characteristics a compound. The permeation is studied from AP to BL in a very simple manner. Used for hit molecule characterisation and to aid lead optimisation.

Permuda
More thorough, but still cost-effective, 2-way permeation study (compared to CacoPilot) including simple P-gp substrate screen (PgpScreen). Used for hit molecule characterisation, lead molecule selection and to aid lead optimisation.

CacoCurve
Comprehensive Caco-2 permeation study giving answers to precise PappAB, involvement of transporters or efflux and intracellular metabolism or accumulation to cells. Used for lead molecule selection and drug candidate characterisation.

SkinPilot
Permeation study on human cadaver skin to characterise compounds and formulations intended for topical administration.

InhibCYP
Cost-effective study to unravel the inhibition potential of NCE towards CYP enzymes. Utilizes cocktail incubation of CYP specific probe compounds. Evaluation of potential drug-drug interactions. Used for lead molecule selection and drug candidate characterisation. See references Turpeinen et al. Eur J Pharm Sci (2005) 24(1), 123; and Tolonen et al. J Mass Spectrom (2007) 42, 960-966.

CYPid
This study pinpoints those CYP enzymes contributing to the production of the metabolites of NCE. Indirect method that utilizes the use of CYP selective inhibitors. Evaluation of potential drug-drug interactions. Used for lead molecule selection and drug candidate characterisation.

reCYPid
As above, to pinpoint metabolizing CYP enzymes, but now the method is direct and utilizes recombinant CYP enzymes. Evaluation of potential drug-drug interactions. Used for lead molecule selection and drug candidate characterisation.

CYPid and reCYPid are complementary: both studies should point to the same direction to be able to reliably state that a certain CYP enzyme produces a certain metabolite. Metabolite profile of NCE should be known before the studies can be performed.

HepatoPlate
Comprehensive metabolism and drug interaction study on fresh or cryopreserved, human or animal hepatocytes in 24-well plate format. Information content includes metabolic stability, metabolite identification, accumulation of parent and metabolites to hepatocyte cells, inhibition and induction of CYP enzymes by parent compound and metabolites. Gives the complete picture of metabolic properties of a compound.


Available species for in vivo studies are mouse, rat, rabbit and dog.
RatPilot
Simple animal-saving determination of tentative bioavailability, Cmax, AUC and T½ of a compound in rat including identification of biotransformations and elucidation tentative metabolite structures.

RatDMPK
Comprehensive but animal-saving determination of oral bioavailability, pharmacokinetics and metabolism of a compound in rat.

NRact
The potential of an NCE to activate PXR and CAR nuclear receptors is evaluated in an in vitro cell-based induction assay. Can be done in human and multiple species. Additionally, a selectivity profile of an NCE with other human nuclear receptors can be tailored.

CytoTox
Straightforward cytotoxicity assay based on mouse hepatocytes. Used for hit molecule characterisation, lead molecule selection and to aid lead optimisation.