in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
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171<br />
proteases [aspartic proteases] ❚<br />
catheps<strong>in</strong> E<br />
❚ Aspartic protease<br />
Ref. 1001<br />
Q 4 weeks<br />
Included <strong>in</strong>:<br />
Organ safety profile<br />
Source<br />
mouse recomb<strong>in</strong>ant (NS0 cells)<br />
Substrate<br />
Mca-PLGL-Dpa-AR-NH 2 (6 µM)<br />
Measured product Mca-peptides<br />
Detection method fluorimetry<br />
Reference<br />
pepstat<strong>in</strong> A (IC 50 : 2.6 nM)<br />
Yasuda, Y. et al. (1999) J. Biochem., 125: 1137-1143.<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<strong>Cerep</strong><br />
services<br />
Receptors<br />
HIV-1 protease<br />
❚ Aspartic protease<br />
Ref. 0346<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 />
Source<br />
human recomb<strong>in</strong>ant (E. coli)<br />
Substrate<br />
antranilyl-HIV (75 µM)<br />
Measured product N-term<strong>in</strong>al tripeptide<br />
Detection method fluorimetry<br />
Reference<br />
pepstat<strong>in</strong> A (IC 50 : 3 µM)<br />
Toth, M.V. and Marshall, G.R. (1990) Int. J. Prote<strong>in</strong> Res., 36: 544-550.<br />
enzyme activity (% of control)<br />
100<br />
50<br />
0<br />
-8 -7 -6 -5 -4 -3<br />
log [drug] (M)<br />
pepstat<strong>in</strong> A<br />
warfar<strong>in</strong><br />
Ion<br />
channels<br />
Transporters<br />
ACE<br />
❚ Metalloprotease<br />
Ref. 0979<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 (mur<strong>in</strong>e cells)<br />
Substrate<br />
Mca-RPPGFSAFK(DNP)-OH (10 µM)<br />
Measured product Mca-peptides<br />
Detection method fluorimetry<br />
Reference<br />
captopril (IC 50 : 3.1 nM)<br />
Hoorn, C.M. and Roth, R.A. (1993) Brit. J. Pharmacol., 110: 597-602.<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
K<strong>in</strong>ases<br />
Epigenetic &<br />
DNA-related<br />
enzymes<br />
ACE<br />
❚ metalloprotease<br />
tissue<br />
Ref. 0302<br />
Q 4 weeks<br />
Source<br />
rabbit aorta<br />
Agonist angiotens<strong>in</strong>-I (pD 2 = 7.9)<br />
Antagonist captopril (pA 2 = 8.7)<br />
Test concentrations<br />
[Solvent] must be kept ≤ 0.1%<br />
3 concentrations, n=2 (2 tissues) for both<br />
activities<br />
Kuroda, K. et al. (1990) Arzneim.-Forsch. Drug Res., 40: 968-973.<br />
tension (% of max.)<br />
100<br />
50<br />
0<br />
-10 -9 -8 -7<br />
log [agonist] (M)<br />
captopril<br />
none<br />
1 nM<br />
3 nM<br />
10 nM<br />
<br />
Other<br />
enzymes<br />
Specialized<br />
cellular<br />
assays<br />
ACE-2<br />
❚ metalloprotease<br />
Ref. 1954<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 />
Substrate<br />
Measured product<br />
Detection method<br />
Reference<br />
human recomb<strong>in</strong>ant (mur<strong>in</strong>e cells)<br />
Mca-YVADPAK(DNP)-OH (10 µM)<br />
Mca-peptides<br />
fluorimetry<br />
AC-GG-26-NH 2 (IC 50 : 400 nM)<br />
Huang, L. et al. (2003) J. Biol. Chem., 278: 15532-15540.<br />
enzyme activity (% of control)<br />
100<br />
50<br />
0<br />
-11 -10 -9 -8 -7 -6 -5 -4 -3 -2<br />
log [drug] (M)<br />
AC-GG-26-NH 2<br />
captopril<br />
EDTA<br />
chloro-2-<br />
benzene<br />
Standard<br />
profiles<br />
Test<strong>in</strong>g<br />
conditions<br />
ECE-1<br />
❚ metalloprotease<br />
Ref. 0184<br />
Q 3 weeks<br />
Included <strong>in</strong>:<br />
Non-k<strong>in</strong>ase enzyme profile<br />
Organ safety profile<br />
Source<br />
human recomb<strong>in</strong>ant (NSO cells)<br />
Substrate<br />
ECE-1 fluorescent substrate (15 µM)<br />
Measured product Mca-RPPGFSA<br />
Detection method fluorimetry<br />
Reference<br />
phosphoramidon (IC 50 : 31 nM)<br />
Ahn, K. et al. (1998) Arch. Biochem. Biophys., 359: 258-268.<br />
enzyme activity (% of control)<br />
100<br />
50<br />
0<br />
-10 -9 -8 -7 -6 -5 -4 -3<br />
log [drug] (M)<br />
phosphoramidon<br />
phenanthrol<strong>in</strong>e<br />
thiorphan<br />
captopril<br />
Order<strong>in</strong>g<br />
<strong>in</strong>formation<br />
Assay list<br />
& <strong>in</strong>dex
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