in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
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172 <strong>in</strong> <strong>vitro</strong> pharmacology <strong>2011</strong> catalog<br />
❚ proteases [metalloproteases]<br />
ECE-1<br />
❚ metalloprotease<br />
tissue<br />
Ref. 0313<br />
Q 4 weeks<br />
Source<br />
rabbit saphenous artery<br />
Agonist big endothel<strong>in</strong>-1 (pD 2 = 8.5)<br />
Antagonist phosphoramidon (pA 2 = 8)<br />
Test concentrations<br />
[Solvent] must be kept ≤ 0.1%<br />
3 concentrations, n=2 (2 tissues)<br />
for both activities<br />
Auguet, M. et al. (1992) Eur. J. Pharmacol., 224: 101-102.<br />
tension (% of max.)<br />
100<br />
50<br />
0<br />
-9 -8 -7<br />
log [agonist] (M)<br />
phosphoramidon<br />
none<br />
0.01 µM<br />
0.1 µM<br />
1 µM<br />
MMP-1<br />
❚ metalloprotease<br />
Ref. 0510<br />
Q 3 weeks<br />
Included <strong>in</strong>:<br />
Non-k<strong>in</strong>ase enzyme profile<br />
BioPr<strong>in</strong>t ® profile<br />
Organ safety profile<br />
Source<br />
human recomb<strong>in</strong>ant (E. coli)<br />
Substrate DNP-P-Cha-GC(Me)-HAK(n-Me-Abz)-NH 2<br />
(10 µM)<br />
Measured product Cys(Me)-HAK(n-Me-Abz)-NH 2<br />
Detection method<br />
Reference<br />
fluorimetry<br />
GM6001 (IC 50 : 1.9 nM)<br />
Bickett, D.A. et al. (1993) Anal. Biochem., 212: 58-64.<br />
enzyme activity (% of control)<br />
100<br />
50<br />
0<br />
-12 -11 -10 -9 -8 -7<br />
log [drug] (M)<br />
GM 6001<br />
TIMP-1<br />
TIMP-2<br />
MMP-2<br />
❚ metalloprotease<br />
Ref. 0489<br />
Q 3 weeks<br />
Included <strong>in</strong>:<br />
BioPr<strong>in</strong>t ® profile<br />
Source<br />
human recomb<strong>in</strong>ant<br />
Substrate<br />
NFF-2 (10 µM)<br />
Measured product Mca-RPKPYA<br />
Detection method fluorimetry<br />
Reference<br />
GM6001 (IC 50 : 1.6 nM)<br />
Nagase, N. et al. (1994) J. Biol. Chem., 269: 20952-20957.<br />
enzyme activity (% of control)<br />
100<br />
50<br />
0<br />
-11 -10 -9 -8 -7<br />
log [drug] (M)<br />
GM 6001<br />
TIMP-2<br />
TIMP-1<br />
MMP-3<br />
❚ metalloprotease<br />
Ref. 0490<br />
Q 3 weeks<br />
Included <strong>in</strong>:<br />
Non-k<strong>in</strong>ase enzyme profile<br />
Source<br />
human recomb<strong>in</strong>ant<br />
Substrate<br />
NFF-2 (10 µM)<br />
Measured product Mca-RPKPYA<br />
Detection method fluorimetry<br />
Reference<br />
GM6001 (IC 50 : 35 nM)<br />
Nagase, N. et al. (1994) J. Biol. Chem., 269: 20952-20957.<br />
enzyme activity (% of control)<br />
100<br />
50<br />
GM 6001<br />
0<br />
TIMP-1<br />
TIMP-2<br />
-12 -11 -10 -9 -8 -7 -6<br />
log [drug] (M)<br />
MMP-7<br />
❚ metalloprotease<br />
Ref. 0502<br />
Q 3 weeks<br />
Source<br />
human recomb<strong>in</strong>ant (E. coli)<br />
Substrate<br />
MMP-2/MMP-7 substrate (5 µM)<br />
Measured product Mca-PLG<br />
Detection method fluorimetry<br />
Reference<br />
GM6001 (IC 50 : 11 nM)<br />
Quesada, A.R. et al. (1997) Cl<strong>in</strong>. Exp. Metastasis, 15: 26-32.<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
MMP-8<br />
❚ metalloprotease<br />
Ref. 0643<br />
Q 6 weeks<br />
Source<br />
human neutrophils<br />
Substrate<br />
Mca-P-Cha-G-Nva-HA-Dpa-NH 2 (1 µM)<br />
Measured product Mca-P-Cha-G<br />
Detection method fluorimetry<br />
Reference<br />
GM6001 (IC 50 : 0.3 nM)<br />
Knauper, V. et al. (1996) J. Biol. Chem., 271: 1544-1550.
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