in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
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79<br />
<strong>Cerep</strong><br />
services<br />
receptors<br />
<br />
Receptors<br />
[Nuclear<br />
receptors]<br />
[Nuclear receptors]<br />
Ion<br />
channels<br />
❚ Steroid nuclear receptors<br />
AR - agonist radioligand<br />
b<strong>in</strong>d<strong>in</strong>g<br />
Ref. 0933<br />
Q 3 weeks<br />
Included <strong>in</strong>:<br />
Diversity profile<br />
BioPr<strong>in</strong>t ® profile<br />
Organ safety profile<br />
Source<br />
Ligand<br />
Kd<br />
Non specific<br />
Reference<br />
ER (non-selective) - agonist radioligand<br />
b<strong>in</strong>d<strong>in</strong>g<br />
Ref. 0152<br />
Q 3 weeks<br />
Included <strong>in</strong>:<br />
Diversity profile<br />
LNCaP cells (cytosol)<br />
[ 3 H]methyltrienolone (1 nM)<br />
0.8 nM<br />
mibolerone (1 µM)<br />
mibolerone (IC 50 : 2.6 nM)<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
Zava, D.T. et al. (1979) Endocr<strong>in</strong>ology, 104: 1007-1012.<br />
[Custom offer] rat prostate model (Ref. 0155), please contact us at customresearch@cerep.com<br />
Source<br />
Ligand<br />
Kd<br />
Non specific<br />
Reference<br />
MCF-7 cells (cytosol)<br />
[ 3 H]estradiol (0.4 nM)<br />
0.2 nM<br />
17-β-estradiol (6 µM)<br />
17-β-estradiol (IC 50 : 0.35 nM)<br />
Kurata, Y. et al. (2005) J. Pharmacol. Exp. Ther., 313: 916-920.<br />
specific b<strong>in</strong>d<strong>in</strong>g (% of control)<br />
100<br />
50<br />
0<br />
<br />
<br />
<br />
-12 -11 -10 -7 -6 -4 -3<br />
-9 -8 -5<br />
<br />
log [drug] (M)<br />
<br />
<br />
<br />
<br />
β<br />
<br />
17-β-estradiol<br />
mibolerone<br />
testosterone<br />
progesterone<br />
Transporters<br />
K<strong>in</strong>ases<br />
Epigenetic &<br />
DNA-related<br />
enzymes<br />
Other<br />
enzymes<br />
Specialized<br />
cellular<br />
assays<br />
ERα - agonist fluoligand<br />
b<strong>in</strong>d<strong>in</strong>g<br />
Ref. 0484<br />
Q 3 weeks<br />
Included <strong>in</strong>:<br />
BioPr<strong>in</strong>t ® profile<br />
Organ safety profile<br />
fluorimetry<br />
Source<br />
Ligand<br />
Kd<br />
Non specific<br />
human recomb<strong>in</strong>ant (Sf9 cells)<br />
fluormone TM ES2 (1 nM)<br />
4 nM<br />
17-β-estradiol (10 µM)<br />
Reference 17-β-estradiol (IC 50 : 18 nM)<br />
Parker, G.J. et al. (2000) J. Biomol. Screen., 5: 77-88.<br />
specific b<strong>in</strong>d<strong>in</strong>g (% of control)<br />
100<br />
50<br />
0<br />
<br />
-10 -9 -8 -7 -6 -5 -4 -3<br />
-11 -10 -9 -8 -7 -6 -5 -4 -3<br />
-12 -11 -10 -9 -8 -7 -6 -5 -4<br />
-13 -12 -11 -10 -9 -8 -7 -6 -5<br />
-9 -8 -7 -6<br />
-10<br />
-10 -7 -9 -8 -6 -5 -4<br />
17-β-estradiol<br />
DES<br />
-12 -10 -9 -7 -6 -4 -3<br />
-11 -8 -5<br />
-9 -8 -6 -5<br />
-10 -7<br />
log -10[drug] -9 (M) -8 -12 -11 -7 -6 -5<br />
-11 -10 -7 -6 -5 -4<br />
-9 -8<br />
Standard<br />
profiles<br />
Test<strong>in</strong>g<br />
conditions<br />
ERb - agonist fluoligand<br />
fluorimetry<br />
Source<br />
human recomb<strong>in</strong>ant (Hi5 cells)<br />
Ligand<br />
fluormone TM ES2 (1 nM)<br />
Kd<br />
4 nM<br />
b<strong>in</strong>d<strong>in</strong>g<br />
Non specific 17-β-estradiol (10 µM)<br />
Ref. 0485<br />
Reference 17-β-estradiol (IC 50 : 13 nM)<br />
Q 4 weeks<br />
Parker, G.J. et al. (2000) J. Biomol. Screen., 5: 77-88.<br />
specific b<strong>in</strong>d<strong>in</strong>g (% of control)<br />
100<br />
50<br />
17-β-estradiol<br />
0<br />
DES<br />
-10 -9 -8 -7 -6 -5<br />
log [drug] (M)<br />
Order<strong>in</strong>g<br />
<strong>in</strong>formation<br />
Assay list<br />
& <strong>in</strong>dex
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