in vitro PHARMACOLOGY 2011 CATALOG - Cerep

177
no synthases ❚
inducible NOS
cellul ar
Ref. 0194
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Source
constitutive NOS (cerebellar)
Ref. 0198
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RAW 264-7 cells
Stimulant
LPS (0.1 µg/mL) + IFN-γ (50 U/mL)
Substrate
endogenous arginine
Measured product
-
NO 2
Detection method photometry
Reference
1400W (IC 50 : 400 nM)
[Solvent] must be kept ≤ 0.3%
Estrada, C. et al. (1992) Biochem. Biophys. Res. Commun., 186: 475-482.
❚ Whole cell assay to test inhibitors of induction and activity of NOS
Source
Substrate
Measured product
Detection method
Reference
rat cerebellum
[ 3 H]arginine (28 nM) + arginine (400 nM)
[ 3 H]citrulline
scintillation counting
L-NMMA (IC 50 : 370 nM)
Bredt, D.S. and Snyder, S.H. (1990) Proc. Natl. Acad. Sci. USA, 87: 682-685.
enzyme activity (% of control)
100
50
0
-8 -7 -6 -5 -4 -3
log [drug] (M)
L-NMMA
L-NAME
L-arginine
aminoguanidine
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services
Receptors
Ion
channels
Transporters
constitutive NOS (endothelial)
Source
HUV-EC-C
Substrate
[ 3 H]arginine (28 nM) + arginine (50 nM)
Measured product [ 3 H]citrulline
Detection method scintillation counting
Ref. 0197
Reference
L-NMMA (IC 50 : 300 nM)
Q 3 weeks
Pollock, J.S. et al. (1991) Proc. Natl. Acad. Sci. USA, 88: 10480-10484.
enzyme activity (% of control)
100
-10 -9 -8 -7 -6 -5 -4
50
-11 -10 -9 -8 -7 -6
-12 -11 -10 -6
-9 -8 -7
L-NMMA
L-arginine
L-NAME
0
aminoguanidine
-8 -7 -6 -5 -4 -3
log [drug] (M)
Kinases
Epigenetic &
DNA-related
enzymes
-10 -9 -8 -7 -6 -5 -4
-10 -8 -7 -6
-11 -9
Other
enzymes
-12 -11 -10 -9 -8 -7 -6
❚ Arachidonic acid metabolism
Specialized
cellular
assays
5-lipoxygenase
❚ lipoxygenase
Ref. 0772
Q 3 weeks
Included in:
Non-kinase enzyme profile
Diversity profile
Source
human recombinant (Sf9 cells) (cytosol)
Substrate
arachidonic acid (25 µM)
Measured product rhodamine 123
Detection method fluorimetry
Reference
NDGA (IC 50 : 400 nM)
Pufahl, R.A. et al. (2007) Anal. biochem., 364: 204-212.
Standard
profiles
Testing
conditions
12-lipoxygenase
❚ lipoxygenase
Ref. 0883
Q 3 weeks
Included in:
Non-kinase enzyme profile
Source
human platelets
Substrate
arachidonic acid (6 µM)
Measured product ferric oxidation of xylenol orange
Detection method photometry
Reference
NDGA (IC 50 : 1.2 µM)
Waslidge, N.B. and Hayes, D.J. (1995) Anal. biochem., 231: 354-358.
enzyme activity (% of control)
100
50
0
NDGA
baicalein
-8 -7 -6 -5
-9
log [drug] (M)
Ordering
information
Assay list
& index