in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
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13<br />
<strong>Cerep</strong><br />
services<br />
receptors<br />
<br />
Receptors<br />
[GPCRs]<br />
[g prote<strong>in</strong>-coupled receptors]<br />
Ion<br />
channels<br />
❚ Adenos<strong>in</strong>e<br />
Transporters<br />
A 1 - antagonist radioligand<br />
b<strong>in</strong>d<strong>in</strong>g<br />
Ref. 0002<br />
Q 3 weeks<br />
Included <strong>in</strong>:<br />
ExpresS Profile<br />
High-throughput profile<br />
Diversity profile<br />
Source<br />
Ligand<br />
Kd<br />
Non specific<br />
Reference<br />
human recomb<strong>in</strong>ant (CHO cells)<br />
[ 3 H]DPCPX (1 nM)<br />
1.7 nM<br />
DPCPX (1 µM)<br />
DPCPX (IC 50 : 1 nM)<br />
Townsend-Nicholson, A. and Schofield, P.R. (1994) J. Biol. Chem., 269: 2373-2376<br />
specific b<strong>in</strong>d<strong>in</strong>g (% of control)<br />
100<br />
50<br />
0<br />
-11 -10 -9 -8 -7 -6 -5 -4<br />
log [drug] (M)<br />
DPCPX<br />
CPA<br />
NECA<br />
CGS 21680<br />
K<strong>in</strong>ases<br />
Epigenetic &<br />
DNA-related<br />
enzymes<br />
A 1 - agonist radioligand<br />
b<strong>in</strong>d<strong>in</strong>g<br />
Ref. 0442<br />
Q 3 weeks<br />
Included <strong>in</strong>:<br />
BioPr<strong>in</strong>t ® profile<br />
Organ safety profile<br />
Source<br />
Ligand<br />
Kd<br />
Non specific<br />
Reference<br />
human recomb<strong>in</strong>ant (CHO cells)<br />
[ 3 H]CCPA (1 nM)<br />
0.7 nM<br />
CPA (10 µM)<br />
CPA (IC 50 : 1.84 nM)<br />
specific b<strong>in</strong>d<strong>in</strong>g (% of control)<br />
100<br />
50<br />
0<br />
-11 -10 -9 -8 -7 -6 -5 -4<br />
CPA<br />
DPCPX<br />
CGS 21680<br />
log [drug] (M)<br />
Rivkees, S.A. et al. (1995) J. Biol. Chem., 270: 20485-20490.<br />
[CUSTOM OFFER] rat cerebral cortex model (Ref. 0001), please contact us at customresearch@cerep.com<br />
Other<br />
enzymes<br />
Specialized<br />
cellular<br />
assays<br />
A 1<br />
cellul ar<br />
Ref. 2814<br />
Ref. 2820<br />
Q 3 weeks<br />
Agonist effect<br />
Antagonist effect<br />
Source<br />
human recomb<strong>in</strong>ant (CHO cells)<br />
Measured product impedance<br />
Detection method cellular dielectric spectroscopy<br />
Agonist effect Control CPA (1 µM)<br />
Reference CPA (EC 50 : 1 nM)<br />
Antagonist effect Stimulant CPA (10 nM)<br />
Reference DPCPX (IC 50 : 39 nM)<br />
Cordeaux, Y. et al. (2004) Brit. J. Pharmacol., 143: 705-714.<br />
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<br />
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<br />
<br />
<br />
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<br />
[Solvent] must be kept 0.1%<br />
<br />
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<br />
Standard<br />
profiles<br />
Test<strong>in</strong>g<br />
conditions<br />
A 1 - <strong>in</strong>verse agonist effect<br />
cellul ar<br />
Ref. 2408<br />
Q 3 weeks<br />
Source<br />
Measured product cAMP<br />
Detection method HTRF<br />
human recomb<strong>in</strong>ant (CHO cells)<br />
Control<br />
CGS 15943 (10 µM)<br />
Reference CGS 15943 (EC 50 : 161 nM)<br />
[Solvent] must be kept ≤ 0.3%<br />
Shryock, J.C. et al. (1998) Mol. Pharmacol., 53: 886-893.<br />
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Order<strong>in</strong>g<br />
<strong>in</strong>formation<br />
Assay list<br />
& <strong>in</strong>dex
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