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in vitro PHARMACOLOGY 2011 CATALOG - Cerep

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183<br />

miscellaneous enzymes ❚<br />

carbonic anhydrase II<br />

Ref. 2572<br />

Q 3 weeks<br />

Source<br />

human erythrocytes<br />

Substrate<br />

4-nitrophenyl acetate (450 µM)<br />

Measured product 4-nitrophenol<br />

Detection method photometry<br />

Reference<br />

acetazolamide (IC 50 : 29 nM)<br />

Iyer, R. et al. (2006) J. Biomol. Screen., 11: 782-791.<br />

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<br />

<br />

<br />

<strong>Cerep</strong><br />

services<br />

Receptors<br />

FAAH (fatty acid amide hydrolase)<br />

Source<br />

human recomb<strong>in</strong>ant (Sf21 cells)<br />

Substrate<br />

AMC arachidonoyl amide (20 µM)<br />

Measured product 7-am<strong>in</strong>o-4-methyl coumar<strong>in</strong><br />

Detection method Fluorimetry<br />

Ref. 2960<br />

Reference<br />

URB597 (IC 50 :90 nM)<br />

Q 3 weeks<br />

Vandevoorde, S. (2008) Curr. Top. Med. Chem., 8: 247-267.<br />

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Ion<br />

channels<br />

Transporters<br />

HMG-CoA reductase<br />

Ref. 0187<br />

Q 6 weeks<br />

Source<br />

Syrian hamster recomb<strong>in</strong>ant (E. coli)<br />

Substrate<br />

Measured product<br />

Detection method<br />

Reference<br />

HMG-CoA (130 µM) <br />

mevalonate<br />

photometry<br />

mevastat<strong>in</strong> (IC 50 : 4.7 µM)<br />

Omhumar, R.V. et al. (1994) J. Biol. Chem., 269: 6810-6814.<br />

enzyme activity (% of control)<br />

100<br />

50<br />

0<br />

-7 -6 -5 -4<br />

log [drug] (M)<br />

<br />

mevastat<strong>in</strong><br />

K<strong>in</strong>ases<br />

Epigenetic &<br />

DNA-related<br />

enzymes<br />

myeloperoxidase<br />

Ref. 0193<br />

Q <strong>in</strong>quire<br />

Source<br />

human leukocytes<br />

Substrate<br />

guaiacol (80 mM)<br />

Measured product tetraguaiacol<br />

Detection method photometry<br />

Reference<br />

NDGA (IC 50 : 5.1 µM)<br />

Desser, R.K. et al. (1972) Arch. Biochem. Biophys., 148: 452-465.<br />

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<br />

-10 -9 -8 -7 -6<br />

-10 -9 -6 -8 -7 -5 -4<br />

<br />

-11 -10 -9 -8 -7 -6<br />

-12 -11 -10 -6<br />

-9 -8 -7<br />

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100<br />

0<br />

<br />

Other<br />

enzymes<br />

Specialized<br />

cellular<br />

assays<br />

tubul<strong>in</strong><br />

Ref. 3274<br />

Q 3 weeks<br />

Source<br />

porc<strong>in</strong>e bra<strong>in</strong><br />

Substrate<br />

GTP (1 mM)<br />

Measured comp. microtubules polymerisation<br />

Detection method fluorimetry<br />

Reference<br />

v<strong>in</strong>blast<strong>in</strong>e (IC 50 :1200 nM)<br />

Bonne, D et al.(1985) J. Biol. Chem., 260: 2819-2825.<br />

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Standard<br />

profiles<br />

Test<strong>in</strong>g<br />

conditions<br />

xanth<strong>in</strong>e oxidase/superoxide O 2<br />

–<br />

scaveng<strong>in</strong>g<br />

Ref. 0276<br />

Q 3 weeks<br />

Included <strong>in</strong>:<br />

BioPr<strong>in</strong>t ® profile<br />

Source<br />

purified xanth<strong>in</strong>e oxidase from bov<strong>in</strong>e milk<br />

Substrate<br />

Measured product<br />

Detection method<br />

Reference<br />

<br />

hypoxanth<strong>in</strong>e (10 µM)<br />

O 2<br />

–<br />

+ uric acid<br />

photometry<br />

allopur<strong>in</strong>ol (IC 50 : 2.37 µM)<br />

McCord, J.K. and Fridovich, I. (1969) J. Biol. Chem., 244: 6049-6055.<br />

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<br />

Order<strong>in</strong>g<br />

<strong>in</strong>formation<br />

Assay list<br />

& <strong>in</strong>dex

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