in vitro PHARMACOLOGY 2011 CATALOG - Cerep

178 in vitro pharmacology 2011 catalog
❚ arachidonic acid metabolism
15-lipoxygenase
Source
soybean
Substrate
arachidonic acid (35 µM)
❚ lipoxygenase
Measured product ferric oxidation of xylenol orange
Ref. 0190
Detection method photometry
Q 3 weeks
Reference
NDGA (IC 50 : 1.1 µM)
Included in:
Organ safety profile
Waslidge, N.B. and Hayes, D.J. (1995) Anal. biochem., 231: 354-358.
enzyme activity (% of control)
100
50
0
-8 -7 -6 -5 -4
log [drug] (M)
NDGA
COX 1
❚ cyclooxigenase
Ref. 0726
Q 3 weeks
Included in:
Non-kinase enzyme profile
BioPrint ® profile
Source
Substrate
Measured product PGE 2
Detection method EIA
Reference
human recombinant (Sf9 cells)
arachidonic acid (4 µM)
diclofenac (IC 50 : 13 nM)
Glaser, K. et al. (1995) Eur. J. Pharmacol., 281: 107-111.
enzyme activity (% of control)
100
-10 -9 -8 -7 -6 -5 -4
50
-11 -10 -9 -8 -7 -6
-12 -11 -10 -7 -6
-9 -8
diclofenac
0
sulindac
indomethacine
-11 -10 -9 -8 -7 -6 -5
log [drug] (M)
COX 2
❚ cyclooxigenase
Ref. 0727
Q 3 weeks
Included in:
Non-kinase enzyme profile
BioPrint ® profile
Organ safety profile
Source
human recombinant (Sf9 cells)
Substrate
arachidonic acid (2 µM)
Measured product PGE 2
Detection method EIA
Reference
NS398 (IC 50 : 68 nM)
Glaser, K. et al. (1995) Eur. J. Pharmacol., 281: 107-111.
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
NS 398
diclofenac
rofecoxib
0
indomethacine
-10 -9 -8 -7 -6 -5 -4
log [drug] (M)
sPLA 2 (Type V)
❚ phospholipase
Ref. 3176
Q 3 weeks
Included in:
Non-kinase enzyme profile
Organ safety profile
Source
Substrate
Measured product
Detection method
human recombinant (E. coli)
diheptanoyl thio-PC (250 µM)
heptanoyl thio-PC
photometry
Reference
oleyloxyethyl phosphorylcholine
(IC 50 : 20 µM)
Tiege, U.J. et al. (2005) J. Lipid. Res., 46: 1604-1614.
sPLA 2 (bee venom type III)
❚ phospholipase
Ref. 2999
Q 3 weeks
Source
Substrate
Measured product
Detection method
Reference
bee venom
diheptanoyl thio-PC (250 µM)
heptanoyl thio-PC
photometry
oleyloxyethyl phosphorylcholine
(IC 50 : 5.7 µM)
Tiege, U.J. et al. (2005) J. Lipid. Res., 46: 1604-1614.
TXA 2 synthetase
❚ TXA 2 synthetase
Ref. 0564
Q 3 weeks
Source
human platelets
Substrate
PGH 2 (10 µM)
Measured product TXB 2
Detection method EIA
Reference
furegrelate (IC 50 : 6 nM)
Wade, M.L. and Fitzpatrick, F.A. (1997) Arch. Biochem. Biophys., 347: 174-180.
enzyme activity (% of control)
100
50
0
furegrelate
-9 -8 -7 -6 -5
-11 -10
log [drug] (M)