in vitro PHARMACOLOGY 2011 CATALOG - Cerep

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48 in vitro pharmacology 2011 catalog ❚ melanocortin MC 3 cellul ar Ref. 0959 Ref. 1755 Q 3 weeks Agonist effect Antagonist effect Source human recombinant (CHO cells) Measured product cAMP Detection method HTRF Agonist effect Control NDP-a-MSH (1 µM) Reference NDP-a-MSH (EC 50 : 2.2 nM) Antagonist effect Stimulant NDP-a-MSH (30 nM) Reference SHU 9119 (IC 50 : 39 nM) Schioth, H.B. et al. (1997) Neuropeptides, 31: 565-571. cAMP modulation (% of control) 100 100 50 50 0 0 -11 -10 -9 -8 -7 -6 -10 -9 -8 -7 -6 -5 log [agonist] (M) log [antagonist] (M) NDP-α-MSH SHU 9119 α-MSH AGRP (83-132) MT-II ACTH [Solvent] must be kept ≤ 0.3% MC 4 - agonist radioligand binding Ref. 0420 Q 3 weeks Included in: ExpresS Profile High-throughput profile Diversity profile BioPrint ® profile Organ safety profile Source Ligand Kd Non specific Reference human recombinant (CHO cells) [ 125 I]NDP-a-MSH (0.05 nM) 0.54 nM NDP-a-MSH (1 µM) NDP-a-MSH (IC 50 : 0.23 nM) Schioth, H.B. et al. (1997) Neuropeptides, 31: 565-571. specific binding (% of control) -12 -11 -12 -11 -11 -10 100 -12 -11 -9 -8 -7 -6 -5 -4 -10 -9 -8 -7 -10 -9 -8 -7 50 -10 -9 -8 -7 -6 -5 -9 -8 -7 -6 -5 -10 -4 0 -11 -10 -9 -8 -7 -6 -5 -4 -13 -12 -11 -10 -9 -8 -7 -6 log [drug] (M) -12 -11 -10 -9 -8 -7 -6 -5 -4 -13 -12 -11 -10 -9 -8 -7 -6 -5 -4 NDP-α-MSH α-MSH AGRP SHU 9119 MC 4 cellul ar Ref. 0699 Ref. 0700 Q 3 weeks Agonist effect Antagonist effect Source human recombinant (CHO cells) Measured product cAMP Detection method HTRF Agonist effect Control NDP-a-MSH (30 nM) Reference NDP-a-MSH (EC 50 : 0.4 nM) Antagonist effect Stimulant NDP-a-MSH (1 nM) Reference SHU 9119 (IC 50 : 0.5 nM) Vanleeuween, D. et al. (2003) J. Biol. Chem., 278: 15935-15940. cAMP modulation (% of control) 100 50 0 -10 -9 -8 -7 -6 -12 -11 -12 -11 -10 -9 -8 -7 log [agonist] (M) NDP-α-MSH α-MSH MT-II 100 [Solvent] must be kept ≤ 0.3% 50 0 log [antagonist] (M) SHU 9119 AGRP (83-132) MC 4 - inverse agonist effect cellul ar Ref. 2423 Q 3 weeks Source Measured product cAMP Detection method HTRF Control Reference [Solvent] must be kept ≤ 0.3% human recombinant (CHO cells) AGRP (83-132) (1 µM) AGRP (83-132) (IC 50 : 3.13 nM) Adan, R.A.H. and Kas, M.J.H. (2003) Trends Pharmacol. Sci., 24: 315-321. -12 -11 -11 -10 -12 -11 -12 -11 -9 -8 -7 -6 -5 -4 -10 -9 -8 -7 -10 -9 -8 -7 -10 -9 -8 -7 -6 -5 -9 -8 -7 -6 -5 -10 -4 -11 -10 -9 -8 -7 -6 -5 -4 -13 -12 -11 -10 -9 -8 -7 -6 -12 -11 -10 -9 -8 -7 -6 -5 -4 MC 5 - agonist radioligand Source human recombinant (CHO cells) Ligand [ 125 I]NDP-a-MSH (0.05 nM) Kd 0.7 nM Non specific NDP-a-MSH (1 µM) binding Reference NDP-a-MSH (IC 50 : 0.68 nM) Ref. 0448 Q 4 weeks Schioth, H.B. et al. (1997) Neuropeptides, 31: 565-571. α α MC 5 cellul ar Ref. 1869 Ref. 1870 Q 3 weeks Agonist effect Antagonist effect Source human recombinant (CHO cells) Measured product cAMP Detection method HTRF Agonist effect Control a-MSH (10 µM) Reference a-MSH (EC 50 : 380 nM) Antagonist effect Stimulant a-MSH (1 µM) Reference AGRP (83-132) (IC 50 : 120 nM) Fathi, Z. et al. (1995) Neurochem. Res., 20: 107-113. cAMP modulation (% of control) 100 50 0 -12 -11 -10 -9 -8 -7 -6 -5 -10 -9 -8 -7 -6 log [agonist] (M) α-MSH ACTH SHU 9119 NDP-α-MSH 100 [Solvent] must be kept ≤ 0.3% 50 0 log [antagonist] (M) AGRP (83-132) -11 -10 -9 -8 -7 -6 -5 -4 -12 -11 -10 -9 -8 -7 -11 -10 -9 -8 -7 -6 -5 -4
49 ❚ melatonin Cerep services MT 1 (ML 1A ) - agonist radioligand binding Ref. 1538 Q 3 weeks Included in: ExpresS Profile High-throughput profile BioPrint ® profile Organ safety profile Source Ligand Kd Non specific Reference human recombinant (CHO cells) [ 125 I]2-iodomelatonin (0.01 nM) 0.04 nM melatonin (1 µM) melatonin (IC 50 : 0.16 nM) Witt-Enderby, P.A. and Dubocovitch, M.L. (1996) Mol. Pharm., 50: 166-174. specific binding (% of control) 100 50 0 -13 -12 -11 -10 -9 -8 -7 -6 -5 -4 log [drug] (M) melatonin 2-iodomelatonin 6-chloromelatonin luzindole Receptors [GPCRs] Ion channels MT 1 (ML 1A ) cellul ar Ref. 2498 Agonist effect Ref. 2500 Antagonist effect Q 3 weeks Source human recombinant (CHO cells) Measured product impedance Detection method cellular dielectric spectroscopy Agonist effect Control melatonin (10 nM) Reference melatonin (EC 50 : 0.22 nM) Antagonist effect Stimulant melatonin (1 nM) Reference luzindole (IC 50 : 680 nM) Browning, C. et al. (2000) Br. J. Pharmacol., 129: 877-886. [Solvent] must be kept 0.1% Transporters Kinases MT 2 (ML 1B ) - agonist radioligand Source human recombinant (CHO cells) Ligand [ 125 I]2-iodomelatonin (0.05 nM) binding Kd 0.085 nM Ref. 1687 Non specific melatonin (1 µM) Q 3 weeks Reference melatonin (IC 50 : 0.18 nM) Included in: Organ safety profile Beresford, I.J.M. et al. (1998) J. Pharmacol. Exp. Ther., 285: 1239-1245. specific binding (% of control) 100 50 melatonin 2-iodomelatonin 4-P-PDOT 0 luzindole -13 -12 -11 -10 -9 -8 -7 -6 log [drug] (M) Epigenetic & DNA-related enzymes Other enzymes MT 2 (ML 1B ) cellul ar Ref. 2092 Agonist effect Ref. 2100 Antagonist effect Q 3 weeks Source human recombinant (CHO cells) Measured product cAMP Detection method HTRF Agonist effect Control melatonin (1 µM) Reference melatonin (EC 50 : 0.25 nM) Antagonist effect Stimulant melatonin (10 nM) Reference unavailable Beresford, I.J.M. et al. (1998) J. Pharmacol. Exp. Ther., 285: 1239-1245. cAMP modulation (% of control) 100 50 0 log [agonist] (M) melatonin 2-iodomelatonin GR 135531 IIK7 [Solvent] must be kept ≤ 0.3% -11 -10 -12 -11 -10 -9 -8 -7 -6 -9 -8 -7 -6 -5 -4 antagonist effect: no graph available ❚ See other Melatonin assays, page 89 Specialized cellular assays Standard profiles -12 -11 -10 -9 -8 -7 ❚ motilin -12 -11 -12 -11 -10 -9 -8 -7 -10 -9 -8 -7 -6 -5 -11 -10 -9 -8 -7 -6 -5 -4 Testing conditions motilin - agonist radioligand binding Ref. 0470 Q 3 weeks Included in: BioPrint ® profile Source Ligand Kd Non specific Reference human recombinant (CHO cells) [ 125 I]motilin (0.05 nM) 0.26 nM [Nleu 13 ]-motilin (1 µM) [Nleu 13 ]-motilin (IC 50 : 1.4 nM) Feighner, S.D. et al. (1999) Science, 284: 2184-2188. -9 -8 -7 -6 -5 -10 -4 specific binding (% of control) 100 50 0 -12 -11 -10 -9 -8 -7 -6 -5 -4 -3 -2 log [drug] (M) ● [Nleu 13 ]-motilin ■ motilin ▲ erythromicin Ordering information Assay list & index
Page 1 and 2: in vitro pharmacology 2011 catalog
Page 3 and 4: Cerep services p. 4 Receptors [GPC
Page 5 and 6: 5 ❚ tool-box for cell-based assay
Page 7 and 8: 7 ❚ profile design Cerep offers a
Page 9 and 10: 9 ❚ data online A powerful web-ba
Page 11 and 12: 11 in vitro pharmacology assays Rec
Page 13 and 14: 13 Cerep services receptors Recept
Page 15 and 16: 15 Adenosine ❚ A 2B - antagonist
Page 17 and 18: 17 alpha 1B - antagonist radioligan
Page 19 and 20: 19 adrenergic ❚ alpha 2C - antago
Page 21 and 22: adrenergic ❚ 21 beta 3 cellul ar
Page 23 and 24: -12 -11 -10 -9 -8 -7 -6 -5 -4 -3 bo
Page 25 and 26: adykinin ❚ 25 B 2 cellul ar Ref.
Page 27 and 28: 27 ❚ cannabinoid CB 1 - agonist r
Page 29 and 30: 29 chemokines ❚ CCR2 cellul ar Re
Page 31 and 32: 31 cholecystokinin ❚ CCK 2 (CCK B
Page 33 and 34: 33 dopamine ❚ D 2S - antagonist r
Page 35 and 36: dopamine ❚ 35 D 5 cellul ar Ref.
Page 37 and 38: 37 Cerep services ❚ Free fatty ac
Page 39 and 40: 39 galanin ❚ GAL 2 - agonist radi
Page 41 and 42: 41 ❚ Growth hormone-releasing hor
Page 43 and 44: 43 H 3 - agonist radioligand Source
Page 45 and 46: 45 leukotrienes ❚ CysLT 2 (LTC 4
Page 47: melanin concentrating hormone ❚
Page 51 and 52: 51 M 2 - antagonist radioligand bin
Page 53 and 54: 53 muscarinic ❚ M 5 - antagonist
Page 55 and 56: 55 NK 3 - agonist radioligand bindi
Page 57 and 58: neuropeptide y ❚ 57 Y 1 cellul a
Page 59 and 60: 59 Cerep services ❚ opioid and op
Page 61 and 62: 61 NOP (ORL1) - agonist radioligand
Page 63 and 64: 63 platelet activating factor ❚ P
Page 65 and 66: 65 prostanoid ❚ EP 4 - agonist ra
Page 67 and 68: 67 proteinase-activated ❚ PAR2 ce
Page 69 and 70: serotonin ❚ 69 5-HT 1A cellul ar
Page 71 and 72: 71 serotonin ❚ 5-HT 2B - agonist
Page 73 and 74: 73 5-HT 7 - agonist radioligand bin
Page 75 and 76: 75 ❚ thyrotropin releasing hormon
Page 77 and 78: 77 ❚ vasopressin Cerep services O
Page 81 and 82: 81 LXRb - agonist radioligand bindi
Page 85 and 86: 85 gaba ❚ GABA A1 (a1, b2, g2) -
Page 87 and 88: 87 glycine (strychnine-insensitive)
Page 89 and 90: 89 ❚ Melatonin MT 3 (ML 2 ) - ago
Page 91 and 92: 91 ❚ Sigma Cerep services sigma (
Page 93 and 94: 93 Cerep services [Voltage-gated ch
Page 95 and 96: voltage-gated channels [K + channel
Page 97 and 98: transient receptor potential channe
Page 99 and 100:
99 kainate - agonist radioligand bi
Page 101 and 102:
101 ❚ purinergic channels Cerep s
Page 103 and 104:
103 Cerep services transporters Rec
Page 105 and 106:
105 norepinephrine ❚ norepinephri
Page 107 and 108:
107 Cerep services Kinases Receptor
Page 109 and 110:
109 DDR2 kinase Ref. 2783 Q 3 weeks
Page 111 and 112:
111 protein-tyrosine kinases [Rtk]
Page 113 and 114:
113 FLT-3 kinase Ref. 2866 Q 3 week
Page 115 and 116:
115 KDR kinase (VEGFR2) Ref. 2864 Q
Page 117 and 118:
117 TRKB Ref. 2902 Q 3 weeks Includ
Page 119 and 120:
119 protein-tyrosine kinases [Ctk]
Page 121 and 122:
121 JAK1 Ref. 2619 Q 3 weeks Includ
Page 123 and 124:
123 TXK Ref. 2786 Q 3 weeks Include
Page 125 and 126:
125 CDK6 (cycD3) Ref. 2909 Q 3 week
Page 127 and 128:
protein-SERINE/THREONINE kinases [C
Page 129 and 130:
129 JNK3 Ref. 2916 Q 3 weeks Includ
Page 131 and 132:
131 CaMK1d Ref. 2922 Q 3 weeks Incl
Page 133 and 134:
133 MAPKAPK2 Ref. 3367 Q 3 weeks I
Page 135 and 136:
135 PhKg1 Ref. 2745 Q 3 weeks Inclu
Page 137 and 138:
137 ❚ protein-SERINE/THREONINE ki
Page 139 and 140:
139 MSK1 Ref. 1724 Q 3 weeks Source
Page 141 and 142:
141 PKCe Ref. 2044 Q 3 weeks PKCz R
Page 143 and 144:
143 ROCK2 Ref. 2884 Q 3 weeks Inclu
Page 145 and 146:
145 COT kinase (MAP3K8) Ref. 2003 Q
Page 147 and 148:
147 MKK6/p38a (mutant active) Ref.
Page 149 and 150:
149 ❚ protein-SERINE/THREONINE ki
Page 151 and 152:
151 RAF-1/MEK1 Ref. 1703 Q 3 weeks
Page 153 and 154:
153 other kinases ❚ MYT1 kinase R
Page 155 and 156:
155 other kinases ❚ TBK1 Ref. 33
Page 157 and 158:
157 Cerep services Epigenetic & DNA
Page 159 and 160:
159 HDACs ❚ HDAC3 Ref. 2083 Q 3 w
Page 161 and 162:
161 HDACs ❚ sirtuin 3 Source Subs
Page 163 and 164:
163 Cerep services Other enzymes Re
Page 165 and 166:
165 phosphatases ❚ phosphatase LA
Page 167 and 168:
167 phosphatase SHP2 (PTPN11) Sourc
Page 169 and 170:
169 caspase-3 ❚ Cysteine protease
Page 171 and 172:
171 proteases [aspartic proteases]
Page 173 and 174:
173 proteases [metalloproteases]
Page 175 and 176:
phosphodiesterases ❚ 175 PDE4A 1
Page 177 and 178:
177 no synthases ❚ inducible NOS
Page 179 and 180:
179 ❚ Monoamine & neurotransmitte
Page 181 and 182:
181 Cerep services ❚ Transduction
Page 183 and 184:
183 miscellaneous enzymes ❚ carbo
Page 185 and 186:
185 Specialized cellular assays The
Page 187 and 188:
187 ion transport systems ❚ Na +
Page 189 and 190:
189 cytokine secretion ❚ IL-2 sec
Page 191 and 192:
191 expression of endothelial adhes
Page 193 and 194:
193 PDGF-stimulated Balb/c 3T3 prol
Page 195 and 196:
195 cerep Standard profiles ExpresS
Page 197 and 198:
197 ❚ Cellular functional GPCR pr
Page 199 and 200:
Cerep standard profiles ❚ 199 Dr
Page 201 and 202:
Cerep standard profiles ❚ 201 Sa
Page 203 and 204:
203 testing conditions Binding, enz
Page 205 and 206:
205 The reference compound for each
Page 207 and 208:
207 ordering information Quotation
Page 209 and 210:
209 REQUESTED COMPOUND INFORMATION
Page 211 and 212:
shipment instructions ❚ 211 For
Page 213 and 214:
213 assay list & index
Page 215 and 216:
215 CDK5/p35 124 CDK6 (cycD3) 125 C
Page 217 and 218:
217 MMP-3 172 MMP-7 172 MMP-8 172 M
Page 219 and 220:
contacts ❚ france [Laboratories]
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