in vitro PHARMACOLOGY 2011 CATALOG - Cerep

168 in vitro pharmacology 2011 catalog
❚ proteases [serine proteases]
elastase
❚ Serine protease
Ref. 0183
Q 3 weeks
Included in:
Non-kinase enzyme profile
Organ safety profile
Source
Substrate
Measured product
Detection method
Reference
human leukocytes
MeOSAAPV-pNa (0.1 mM)
pNa
photometry
3’,4’dichloroisocoumarin (IC 50 : 392 nM)
Adeyemi, E.O. et al. (1990) J. Pharm. Pharmacol., 42: 487-490.
enzyme activity (% of control)
100
50
0
-8 -7 -6 -5 -4 -3
log [drug] (M)
3',4'dichloroisocoumarin
PMSF
NDGA
HNE (human neutrophil elastase)
Source
human serum
Substrate
elastin fluorescein (1 mg)
Measured product fluorescein
❚ Serine protease
Detection method fluorimetry
Ref. 0562
Reference
3’,4’dichloroisocoumarin (IC 50 : 520 nM)
Q 4 weeks
McGillivray, D. H. et al. (1981) Clin. Chim. Acta., 111: 289-294.
enzyme activity (% of control)
100
50
3',4'dichloroisocoumarin
0
PMSF
-11 -10 -9 -8 -7 -6 -5 -4 -3 -2
log [drug] (M)
kallikrein
❚ Serine protease
Ref. 0791
Q 4 weeks
Included in:
Organ safety profile
Source
human plasma
Substrate
HDPFR-pNa (50 µM)
Measured product pNa
Detection method photometry
Reference
soybean trypsin inhibitor (IC 50 : 6 nM)
Nagase, H and Barrett, A.J. (1981) Biochem. J., 193: 187-192.
tryptase
❚ Serine protease
Ref. 0512
Q 3 weeks
Included in:
Non-kinase enzyme profile
Organ safety profile
Source
human lung
Substrate
N-p-Tosyl-GPR-pNa (0.1 mM)
Measured product pNa
Detection method photometry
Reference
leupeptin (IC 50 : 1 µM)
Schwartz, L.B. and Bradford, T.R. (1986) J. Biol. Chem., 261: 7372-7379.
caspase-1
100
❚ Cysteine protease
Ref. 3251
Q 3 weeks
Source
human recombinant (E. coli)
Substrate
benzyloxycarbonyl-YVAD-AFC (7.5 µM)
Measured product AFC
Detection method fluorimetry
Reference
Ac-YVAD-CHO (IC 50 : 20 nM)
Margolin, N. et al.(1997) J. Biol. Chem., 272: 7223-7228.
enzyme activity (% of control)
50
0
-10 -9 -8 -7 -6 -5 -4
log [drug] (M)
Ac-YVAD-CHO
Ac-DEVD-CHO
Ac-LEHD-CHO
Ac-IETD-CHO
caspase-2
❚ Cysteine protease
Ref. 0681
Q 6 weeks
Source
human recombinant (E. coli)
Substrate
benzyloxycarbonyl-VDVAD-AFC (10 µM)
Measured product AFC
Detection method fluorimetry
Reference
Ac-VDVAD-CHO (IC 50 : 130 nM)
Talanian, R.V. et al. (1997) J. Biol. Chem., 272: 9677-9682.
-10 -9 -8 -7 -6 -5 -4 -3
-11
-10 -9 -8 -7 -6 -5 -4 -3
-12 -11 -10 -9 -8 -7 -6 -5 -4
-11 -10 -9 -8 -7 -6 -5 -4 -3 -2
-10 -9 -8 -7 -6
-10 -9 -8 -7 -6 -5
-4
-12 -11 -10 -9
-8 -7 -6 -5 -4 -3
-12 -11 -10 -9 -8 -7 -6 -5
-11
-10 -9 -8 -7 -6 -5 -4