in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
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78 <strong>in</strong> <strong>vitro</strong> pharmacology <strong>2011</strong> catalog<br />
❚ vasopress<strong>in</strong><br />
V 1b - agonist radioligand<br />
b<strong>in</strong>d<strong>in</strong>g<br />
Ref. 0588<br />
Q 3 weeks<br />
Included <strong>in</strong>:<br />
Organ safety profile<br />
V 2 - agonist radioligand<br />
b<strong>in</strong>d<strong>in</strong>g<br />
Ref. 0497<br />
Q 3 weeks<br />
Included <strong>in</strong>:<br />
Diversity profile<br />
BioPr<strong>in</strong>t ® profile<br />
Source<br />
Ligand<br />
Kd<br />
Non specific<br />
Reference<br />
human recomb<strong>in</strong>ant (CHO cells)<br />
[ 3 H]AVP (0.1 nM)<br />
0.1 nM<br />
AVP (0.1 µM)<br />
AVP (IC 50 : 0.33 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<br />
log [drug] (M)<br />
Tahara, A. et al. (1998) Brit. J. Pharmacol., 125: 1463-1470.<br />
[custom offer] rat cDNA model (Ref. 0466), please contact us at customresearch@cerep.com<br />
Source<br />
Ligand<br />
Kd<br />
Non specific<br />
Reference<br />
human recomb<strong>in</strong>ant (CHO cells)<br />
[ 3 H]AVP (0.3 nM)<br />
0.76 nM<br />
AVP (1 µM)<br />
AVP (IC 50 : 0.954 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 />
log [drug] (M)<br />
AVP<br />
[d(CH 2<br />
) 51<br />
,Tyr(Me) 2<br />
]<br />
-AVP<br />
oxytoc<strong>in</strong><br />
SR 49059<br />
AVP<br />
[d(CH 2 ) 51 ,Tyr(Me) 2 ]<br />
-AVP<br />
SR 121463B<br />
oxytoc<strong>in</strong><br />
Tahara, A. et al. (1998) Brit. J. Pharmacol., 125: 1463-1470.<br />
[custom offer] porc<strong>in</strong>e LLC-PK1 cells model (Ref. 0160), please contact us at customresearch@cerep.com<br />
V 2<br />
cellul ar<br />
Ref. 0237<br />
Ref. 0569<br />
Q 3 weeks<br />
Agonist effect<br />
Antagonist effect<br />
Source<br />
human recomb<strong>in</strong>ant (CHO cells)<br />
Measured product cAMP<br />
Detection method HTRF<br />
Agonist effect Control AVP (1 nM)<br />
Reference AVP (EC 50 : 0.013 nM)<br />
Antagonist effect Stimulant AVP (0.03 nM)<br />
Reference [adamantaneacetyl 1 ,O-Et-D-<br />
Tyr 2 ,Val 4 ,am<strong>in</strong>obutyryl 6 ]-AVP<br />
(IC 50 : 30 nM)<br />
Cotte, N. et al. (1998) J. Biol. Chem., 273: 29462-29468.<br />
cAMP modulation (% of control)<br />
100<br />
100<br />
50<br />
50<br />
0<br />
0<br />
-13 -12 -11 -10 -9 -8 -7 -6 -10 -9 -8 -7 -6 -5<br />
log [agonist] (M)<br />
log [antagonist] (M)<br />
AVP<br />
[adamantaneacetyl 1 ,O-Et-D<br />
Val 4 -dDAVP<br />
-Tyr 2 ,-Val 4 ,am<strong>in</strong>obutyryl 6 ]-AVP<br />
dDAVP<br />
SR 121463B<br />
oxytoc<strong>in</strong><br />
[d(CH 2 ) 51 ,Tyr(Me) 2 ]-AVP<br />
[Solvent] must be kept ≤ 0.3%<br />
-11 -10<br />
-9 -8 -7 -6 -5 -4<br />
-12 -11<br />
-10 -9 -8 -7<br />
-11 -10 -9 -8 -7 -6 -5 -4<br />
-13 -12 -11 -10 -9 -8 -7 -6<br />
-12 -11<br />
-10 -9 -8 -7<br />
-12 -11<br />
-10 -9 -8 -7 -6 -5<br />
-12 -11 -10 -9 -8 -7 -6 -5 -4<br />
-9 -8 -7 -6 -5<br />
-10 -4<br />
For further details and updated <strong>in</strong>formation on assays:<br />
❚ Please go to www.cerep.com catalog onl<strong>in</strong>e or contact us at sales@cerep.com<br />
❚ Europe: +33 (0)5 49 89 30 00 – USA: +1 (425) 895 8666 – Japan: +81 (0)3 3354 4026 – Ch<strong>in</strong>a: +86 21 5132 0568<br />
Assay developed <strong>in</strong> 2010 New assay conditions Human Q Standard turnaround time
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