in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
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48 <strong>in</strong> <strong>vitro</strong> pharmacology <strong>2011</strong> catalog<br />
❚ melanocort<strong>in</strong><br />
MC 3<br />
cellul ar<br />
Ref. 0959<br />
Ref. 1755<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 NDP-a-MSH (1 µM)<br />
Reference NDP-a-MSH (EC 50 : 2.2 nM)<br />
Antagonist effect Stimulant NDP-a-MSH (30 nM)<br />
Reference SHU 9119 (IC 50 : 39 nM)<br />
Schioth, H.B. et al. (1997) Neuropeptides, 31: 565-571.<br />
cAMP modulation (% of control)<br />
100<br />
100<br />
50<br />
50<br />
0<br />
0<br />
-11 -10 -9 -8 -7 -6 -10 -9 -8 -7 -6 -5<br />
log [agonist] (M)<br />
log [antagonist] (M)<br />
NDP-α-MSH<br />
SHU 9119<br />
α-MSH<br />
AGRP (83-132)<br />
MT-II<br />
ACTH<br />
[Solvent] must be kept ≤ 0.3%<br />
MC 4 - agonist radioligand<br />
b<strong>in</strong>d<strong>in</strong>g<br />
Ref. 0420<br />
Q 3 weeks<br />
Included <strong>in</strong>:<br />
ExpresS Profile<br />
High-throughput profile<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 />
human recomb<strong>in</strong>ant (CHO cells)<br />
[ 125 I]NDP-a-MSH (0.05 nM)<br />
0.54 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 />
specific b<strong>in</strong>d<strong>in</strong>g (% of control)<br />
-12 -11<br />
-12 -11<br />
-11 -10<br />
100<br />
-12 -11<br />
-9 -8 -7 -6 -5 -4<br />
-10 -9 -8 -7<br />
-10 -9 -8 -7<br />
50 -10 -9 -8 -7 -6 -5<br />
-9 -8 -7 -6 -5<br />
-10 -4<br />
0<br />
-11 -10<br />
-9 -8 -7 -6 -5 -4<br />
-13 -12 -11 -10 -9 -8 -7 -6<br />
log [drug] (M)<br />
-12 -11 -10 -9 -8 -7 -6 -5 -4<br />
-13 -12 -11 -10 -9 -8 -7 -6 -5 -4<br />
NDP-α-MSH<br />
α-MSH<br />
AGRP<br />
SHU 9119<br />
MC 4<br />
cellul ar<br />
Ref. 0699<br />
Ref. 0700<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 NDP-a-MSH (30 nM)<br />
Reference NDP-a-MSH (EC 50 : 0.4 nM)<br />
Antagonist effect Stimulant NDP-a-MSH (1 nM)<br />
Reference SHU 9119 (IC 50 : 0.5 nM)<br />
Vanleeuween, D. et al. (2003) J. Biol. Chem., 278: 15935-15940.<br />
cAMP modulation (% of control)<br />
100<br />
50<br />
0<br />
-10 -9 -8 -7 -6 -12 -11<br />
-12 -11 -10 -9 -8 -7<br />
log [agonist] (M)<br />
NDP-α-MSH<br />
α-MSH<br />
MT-II<br />
100<br />
[Solvent] must be kept ≤ 0.3%<br />
50<br />
0<br />
log [antagonist] (M)<br />
SHU 9119<br />
AGRP (83-132)<br />
MC 4 - <strong>in</strong>verse agonist effect<br />
cellul ar<br />
Ref. 2423<br />
Q 3 weeks<br />
Source<br />
Measured product cAMP<br />
Detection method HTRF<br />
Control<br />
Reference<br />
[Solvent] must be kept ≤ 0.3%<br />
human recomb<strong>in</strong>ant (CHO cells)<br />
AGRP (83-132) (1 µM)<br />
AGRP (83-132) (IC 50 : 3.13 nM)<br />
Adan, R.A.H. and Kas, M.J.H. (2003) Trends Pharmacol. Sci., 24: 315-321.<br />
<br />
-12 -11<br />
-11 -10<br />
-12 -11<br />
<br />
<br />
-12 -11<br />
-9 -8 -7 -6 -5 -4<br />
-10 -9 -8 -7<br />
-10 -9 -8 -7<br />
-10 -9 -8 -7 -6 -5<br />
<br />
-9 -8 -7 -6 -5<br />
-10 -4<br />
<br />
-11 -10<br />
-9 -8 -7 -6 -5 -4<br />
-13 -12 -11 -10 -9 -8 -7 -6<br />
<br />
-12 -11 -10 -9 -8 -7 -6 -5 -4<br />
<br />
<br />
<br />
MC 5 - agonist radioligand<br />
Source<br />
human recomb<strong>in</strong>ant (CHO cells)<br />
Ligand<br />
[ 125 I]NDP-a-MSH (0.05 nM)<br />
Kd<br />
0.7 nM<br />
Non specific NDP-a-MSH (1 µM)<br />
b<strong>in</strong>d<strong>in</strong>g<br />
Reference NDP-a-MSH (IC 50 : 0.68 nM)<br />
Ref. 0448<br />
Q 4 weeks<br />
Schioth, H.B. et al. (1997) Neuropeptides, 31: 565-571.<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
<br />
α<br />
α<br />
<br />
<br />
MC 5<br />
cellul ar<br />
Ref. 1869<br />
Ref. 1870<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 a-MSH (10 µM)<br />
Reference a-MSH (EC 50 : 380 nM)<br />
Antagonist effect Stimulant a-MSH (1 µM)<br />
Reference AGRP (83-132) (IC 50 : 120 nM)<br />
Fathi, Z. et al. (1995) Neurochem. Res., 20: 107-113.<br />
cAMP modulation (% of control)<br />
100<br />
50<br />
0<br />
-12 -11 -10 -9 -8 -7 -6 -5 -10 -9 -8 -7 -6<br />
log [agonist] (M)<br />
α-MSH<br />
ACTH<br />
SHU 9119<br />
NDP-α-MSH<br />
100<br />
[Solvent] must be kept ≤ 0.3%<br />
50<br />
0<br />
log [antagonist] (M)<br />
AGRP (83-132)<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