in vitro PHARMACOLOGY 2011 CATALOG - Cerep

209
REQUESTED COMPOUND INFORMATION ❚
Remarks for ADME-Tox assays:
- Any study including mass spectrometry (MS) assays (such as stability, permeability, protein binding) requires both molecuular
weight (MW) and formula weight (FW) of each tested compound, even if they are the same. The FW is required to prepare
the stock solution of each compound at the correct concentration. The MW gives indication on which expected molecular ion
to look for in the LC-MS analysis of samples.
- Chemical structure or list of the ionizable groups is required for ionization constant (pKa) assay.
- Solubility information is useful and recommended for pKa and genotoxicity testing (due to high test concentrations).
Warning: Cerep will apply the standard solubilization process described in the flow chart below when compounds are received
at the testing site, unless special instructions are provided with the compounds.
Customized handling procedure of compounds can be accommodated, please inquire for pricing conditions.
Cerep
services
Receptors
cerep compound management process
Standard solubilization process
[diagram]
DMSO solvents are stored
under nitrogen to minimize
potential oxidation and water
absorption.
NOTE: Covaris: this device sends
acoustic energy waves from a
transducer that converges and
focuses on a small area. Covaris
processing of compounds is done
isothermally maintaining temperature
between 20 and 25°C.
Dedicated team
Daily dilutions in 100% fresh DMSO
Only 1 freeze/thaw cycle in standard
process to minimize precipitation
Constant concentration of solvent
in the assays
Cherry-picking and multiplexing
expertise
Customized handling procedure of
compounds upon request
POWDER
FORM
more
Weighing in a glass tube
Solubilization at 10 mM
in DMSO
Covaris processing
NO
Diluted down to 5 mM in DMSO
Covaris processing
NO
Diluted down to 1 mM in DMSO
Covaris processing
NO
less
YES
YES
YES
less
Solubilization in client's vial
(except for 1 dram glass vial)
Solubilization at 10 mM in DMSO
Vortexing 10 min
Solubilization in client's vial
(when in 1 dram glass vial)
Solubilization at 10 mM
in DMSO
Covaris processing
YES
Ready to be dispatched
in aliquots storage
at -20°C
Study interrupted - Client contacted
NO
Sonication
YES
NO
Diluted down to 5 mM in DMSO
Vortexing 10 min
YES
NO
Diluted down to 1 mM in DMSO
Vortexing 10 min
YES
NO
Ion
channels
Transporters
Kinases
Epigenetic &
DNA-related
enzymes
Other
enzymes
❚ sample size [minimum compound amount - including IC 50 /EC 50 follow-up studies]
❚
Binding, enzyme and cellular assays
Assuming a molecular weight ≤ 500 g/mol and a testing concentration of 10 µM in duplicate (including a possible retest).
Screening
Screening + Follow up
with highest concentration at 10 µM 1
Weight (pre-weighed) Volume (100% DMSO) Weight (pre-weighed) Volume (100% DMSO)
Individual binding, enzyme and cellular catalog assays
1 to 3 assays 1 mg 25 µL @ 10 mM 1 mg 60 µL @ 10 mM
4 to 5 assays 1 mg 35 µL @ 10 mM 1 mg 70 µL @ 10 mM
6 to 10 assays 1 mg 50 µL @ 10 mM 1 mg 100 µL @ 10 mM
11 to 15 assays 1 mg 65 µL @ 10 mM 1 mg 110 µL @ 10 mM
16 to 20 assays 1 mg 75 µL @ 10 mM 1 mg 125 µL @ 10 mM
21 to 40 assays 1 mg 100 µL @ 10 mM 1.5 mg 250 µL @ 10 mM
41 to 50 assays 1 mg 150 µL @ 10 mM 2 mg 275 µL @ 10 mM
51 to 70 assays 1.5 mg 225 µL @ 10 mM 2.5 mg 400 µL @ 10 mM
71 to 100 assays 2 mg 300 µL @ 10 mM 3 mg 550 µL @ 10 mM
101 to 135 assays 2 mg 350 µL @ 10 mM 4 mg 650 µL @ 10 mM
136 to 150 assays 2.5 mg 400 µL @ 10 mM 4 mg 750 µL @ 10 mM
151 to 200 assays 3 mg 500 µL @ 10 mM 5 mg 1000 µL @ 10 mM
201 to 250 assays 3.5 mg 600 µL @ 10 mM inquire inquire
1 Assuming ~10% of test in IC 50 . Usually, for 1 IC 50 : 30 µL @ 10 mM and + 25 µL @ 10 mM by additional IC 50 .
Specialized
cellular
assays
Standard
profiles
Testing
conditions
Ordering
information
Assay list
& index