in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
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melan<strong>in</strong> concentrat<strong>in</strong>g hormone ❚<br />
47<br />
MCH 2<br />
cellul ar<br />
Ref. 1106<br />
Ref. 1107<br />
Q 3 weeks<br />
Agonist effect<br />
Antagonist effect<br />
Source<br />
human recomb<strong>in</strong>ant (CHO cells)<br />
Measured product <strong>in</strong>tracellular [Ca 2+ ]<br />
Detection method fluorimetry<br />
Agonist effect Control human MCH (100 nM)<br />
Reference human MCH (EC 50 : 4.2 nM)<br />
Antagonist effect Stimulant human MCH (30 nM)<br />
Reference unavailable<br />
Wang, S. et al. (2001) J. Biol. Chem., 276: 34664-34670.<br />
Ca 2+ mobilization (% of control)<br />
100<br />
50<br />
0<br />
-11 -10<br />
-9 -8 -7 -6<br />
log [agonist] (M)<br />
human MCH<br />
[Phe 13 ,Tyr 19 ]-MCH<br />
salmon MCH<br />
[Solvent] must be kept ≤ 0.1%<br />
antagonist effect:<br />
no graph available<br />
<strong>Cerep</strong><br />
services<br />
<br />
Receptors<br />
[GPCRs]<br />
-11 -10<br />
-9 -8 -7 -6 -5 -4<br />
-12 -11<br />
-10 -9 -8 -7<br />
-11 -10<br />
-9 -8 -7 -6 -5 -4<br />
-12 -11 -10 -9 -8 -7 -6 -5 -4 -3<br />
-12 -11<br />
-12 -11<br />
-10 -9 -8 -7<br />
-10 -9 -8 -7 -6 -5<br />
Ion<br />
channels<br />
-9 -8 -7 -6 -5<br />
-10 -4<br />
❚ melanocort<strong>in</strong><br />
MC 1 - agonist radioligand<br />
b<strong>in</strong>d<strong>in</strong>g<br />
Ref. 0644<br />
Q 3 weeks<br />
Included <strong>in</strong>:<br />
BioPr<strong>in</strong>t ® profile<br />
Source<br />
Ligand<br />
Kd<br />
Non specific<br />
Reference<br />
B16-F1 cells (endogenous)<br />
[ 125 I]NDP-a-MSH (0.05 nM)<br />
0.05 nM<br />
NDP-a-MSH (1 µM)<br />
NDP-a-MSH (IC 50 : 0.18 nM)<br />
Siegrist, W. et al. (1988) J. Recep. Res., 8: 323-343.<br />
specific b<strong>in</strong>d<strong>in</strong>g (% of control)<br />
100<br />
50<br />
NDP-α-MSH<br />
α-MSH<br />
MT-II<br />
0<br />
ACTH<br />
-12 -11 -10 -9 -8 -7 -6<br />
log [drug] (M)<br />
Transporters<br />
K<strong>in</strong>ases<br />
Epigenetic &<br />
DNA-related<br />
enzymes<br />
MC 1<br />
cellul ar<br />
Ref. 2147<br />
Ref. 2148<br />
Q 3 weeks<br />
Agonist effect<br />
Antagonist effect<br />
Source<br />
B16-F1 cells (endogenous)<br />
Measured product cAMP<br />
Detection method HTRF<br />
Agonist effect Control NDP-a-MSH (1 µM)<br />
Reference NDP-a-MSH (EC 50 : 1.2 nM)<br />
Antagonist effect Stimulant NDP-a-MSH (10 nM)<br />
Reference AGRP (83-132) (IC 50 : 248 nM)<br />
Tatro, J.B. et al. (1990) Cancer Research., 50: 1237-1242.<br />
cAMP modulation (% of control)<br />
100<br />
50<br />
0<br />
-12 -11<br />
-10 -9 -8 -7 -6 -5<br />
log [agonist] (M)<br />
NDP-α-MSH<br />
α-MSH<br />
ACTH (1-39)<br />
MT-II<br />
100<br />
[Solvent] must be kept ≤ 0.3%<br />
50<br />
0<br />
-12 -11<br />
-10 -9 -8 -7 -6 -5<br />
log [antagonist] (M)<br />
AGRP (83-132)<br />
SHU 9119<br />
HS 024<br />
Other<br />
enzymes<br />
Specialized<br />
cellular<br />
assays<br />
MC 2<br />
cellul ar<br />
Ref. 2240<br />
Ref. 2241<br />
Q 3 weeks<br />
Agonist effect<br />
Antagonist effect<br />
Source<br />
human recomb<strong>in</strong>ant (Cloudman M3 cells)<br />
Measured product cAMP<br />
Detection method HTRF<br />
Agonist effect Control ACTH (1-39) (1 µM)<br />
Reference ACTH (1-39) (EC 50 : 14 nM)<br />
Antagonist effect Stimulant ACTH (1-39) (30 nM)<br />
Reference unavailable<br />
Kapas, S. et al. (1996) Endocr<strong>in</strong>ol., 137: 3291-3294.<br />
<br />
-12 -11<br />
-12 -11<br />
-12 -11<br />
<br />
<br />
-10 -9 -8 -7<br />
-10 -9 -8 -7<br />
-10 -9 -8 -7 -6 -5<br />
<br />
-11 -10<br />
-9 -8 -7<br />
-6 -5 -10 -4 <br />
<br />
<br />
<br />
α<br />
α<br />
[Solvent] must be kept 0.3%<br />
-9 -8 -7 -6 -5 -4<br />
-13 -12 -11 -10 <br />
-9 -8 -7 -6<br />
<br />
-12 -11 -10 -9 -8 -7 -6 -5 -4<br />
Standard<br />
profiles<br />
Test<strong>in</strong>g<br />
conditions<br />
-11 -10<br />
-9 -8 -7 -6 -5 -4<br />
MC 3 - agonist radioligand<br />
b<strong>in</strong>d<strong>in</strong>g<br />
Ref. 0447<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 />
[ 125 I]NDP-a-MSH (0.075 nM)<br />
0.4 nM<br />
NDP-a-MSH (1 µM)<br />
NDP-a-MSH (IC 50 : 0.23 nM)<br />
Schioth, H.B. et al. (1997) Neuropeptides, 31: 565-571.<br />
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α<br />
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α<br />
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Order<strong>in</strong>g<br />
<strong>in</strong>formation<br />
Assay list<br />
& <strong>in</strong>dex