in vitro PHARMACOLOGY 2011 CATALOG - Cerep

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72 in vitro pharmacology 2011 catalog ❚ serotonin 5-HT 4e - antagonist radioligand binding Ref. 0501 Q 3 weeks Included in: BioPrint ® profile Organ safety profile Source Ligand Kd Non specific Reference human recombinant (CHO cells) [ 3 H]GR 113808 (0.3 nM) 0.15 nM serotonin (100 µM) serotonin (IC 50 : 170 nM) Mialet, J. et al. (2000) Brit. J. Pharmacol., 129: 771-781. specific binding (% of control) 100 50 0 -11 -10 -9 -8 -7 -6 -5 -4 log [drug] (M) serotonin GR 113808 ketanserin 8-OH-DPAT 5-HT 4e cellul ar Ref. 1044 Ref. 1045 Q 3 weeks Included in: Agonist effect Antagonist effect Cellular functional GPCR profile Source human recombinant (CHO cells) Measured product cAMP Detection method HTRF Agonist effect Control serotonin (1 µM) Reference serotonin (EC 50 : 5.2 nM) Antagonist effect Stimulant serotonin (30 nM) Reference GR 113808 (IC 50 : 0.3 nM) Mialet, J. et al. (2000) Brit. J. Pharmacol., 129: 771-781. cAMP modulation (% of control) 100 100 50 50 0 0 -11 -10 -9 -8 -7 -6 -5 -4 -3 -12 -11 -10 -9 -8 -7 -6 -5 -4 -3 log [agonist] (M) log [antagonist] (M) serotonin GR 113808 RS 67506 ketanserin cisapride 5-CT 5-HT 4 tissue Ref. 0336 Q 4 weeks Source guinea-pig colon Agonist serotonin (pD 2 = 7.1) Antagonist GR 113808 (pA 2 = 9.7) Test concentrations 3 concentrations, n=2 (2 tissues) for both activities [Solvent] must be kept ≤ 0.1% Gale, J.D. et al. (1994) Brit. J. Pharmacol., 111: 332-338. tension (% of max.) -12 -11 -12 -11 -11 -10 -9 -8 -7 -6 -5 -4 -12 -11 -10 -9 -8 -7 100 -11 -10 -9 -8 -7 -6 -5 -4 -10 -9 -8 -7 50 -10 -9 -8 -7 -6 -5 -10 -9 -8 -7 -6 -5 -4 GR 113808 none 1 nM 3 nM 0 10 nM -9 -8 -7 -6 -5 -4 log [agonist] (M) 5-HT 5a - agonist radioligand binding Ref. 0140 Q 3 weeks Included in: ExpresS Profile High-throughput profile Organ safety profile Source Ligand Kd Non specific Reference human recombinant (HEK-293 cells) [ 3 H]LSD (1.5 nM) 1.5 nM serotonin (100 µM) serotonin (IC 50 : 120 nM) Rees, S. et al. (1994) FEBS Lett., 355: 242-246. specific binding (% of control) 100 50 0 -11 -10 -9 -8 -7 -6 -5 -4 -3 log [drug] (M) serotonin methiothepin 8-OH-DPAT ketanserin 5-HT 6 - agonist radioligand binding Ref. 0142 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) [ 3 H]LSD (2 nM) 1.8 nM serotonin (100 µM) serotonin (IC 50 : 150 nM) specific binding (% of control) 100 50 0 -11 -10 -9 -8 -7 -6 -5 -4 log [drug] (M) Monsma, F.J. et al. (1993) Mol. Pharmacol., 43: 320-327. [custom offer] rat cDNA model (Ref. 0141), please contact us at customresearch@cerep.com serotonin methiothepin MDL 72222 8-OH-DPAT 5-HT 6 cellul ar Ref. 1627 Ref. 1628 Q 3 weeks Included in: Agonist effect Antagonist effect Cellular functional GPCR profile Source human recombinant (CHO cells) Measured product cAMP Detection method HTRF Agonist effect Control serotonin (10 µM) Reference serotonin (EC 50 : 20 nM) Antagonist effect Stimulant serotonin (100 nM) Reference methiothepin (IC 50 : 65 nM) Kohen, R. et al. (1996) J. Neurochem., 66: 47-56. cAMP modulation (% of control) 100 50 0 -11 -10 -9 -8 -7 -6 -5 -4 log [agonist] (M) serotonin 5-methoxytryptamine 5-CT 100 50 0 -10 -9 -8 -7 -6 -5 log [antagonist] (M) methiothepin SB 285585 Ro 046790 -11 -10 -9 -8 -7 -6 -5 -4 -12 -11 -10 -9 -8 -7
73 5-HT 7 - agonist radioligand binding Ref. 0144 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) [ 3 H]LSD (4 nM) 2.3 nM serotonin (10 µM) serotonin (IC 50 : 0.45 nM) specific binding (% of control) 100 50 0 -11 -10 -9 -8 -7 -6 -5 -4 serotonin ❚ log [drug] (M) Shen, Y. et al. (1993) J. Biol. Chem., 268: 18200-18204. [custom offer] rat cDNA model (Ref. 0143), please contact us at customresearch@cerep.com serotonin 8-OH-DPAT ketanserin MDL 72222 Cerep services Receptors [GPCRs] 5-HT 7 cellul ar Ref. 1661 Ref. 1662 Q 3 weeks Included in: Agonist effect Antagonist effect Cellular functional GPCR profile Source human recombinant (CHO cells) Measured product cAMP Detection method HTRF Agonist effect Control serotonin (10 µM) Reference serotonin (EC 50 : 25 nM) Antagonist effect Stimulant serotonin (300 nM) Reference mesulergine (IC 50 : 25 nM) Adham, N. et al. (1998) J. Pharmacol. Exp. Ther., 287: 508-514. ❚ See other Serotonin assays pp. 91, 101 and 105 ❚ For sigma assays, see "Other receptors", page 91 Ion channels Transporters ❚ somatostatin Kinases sst (non-selective) - agonist radioligand binding Ref. 0149 Q 3 weeks Included in: ExpresS Profile High-throughput profile Source Ligand Kd Non specific Reference AtT-20 cells [ 125 I]Tyr 11 -somatostatin-14 (0.05 nM) 0.08 nM somatostatin-14 (300 nM) somatostatin-14 (IC 50 : 0.2 nM) Brown, P.J. et al. (1990) J. Biol. Chem., 265: 17995-18004. specific binding (% of control) 100 50 0 -12 -11 -10 -9 -8 -7 log [drug] (M) somatostatin-14 [D-Trp 8 ]- somatostatin somatostatin-28 BIM 23056 Epigenetic & DNA-related enzymes Other enzymes sst 1 - agonist radioligand binding Ref. 1940 Q 3 weeks Included in: BioPrint ® profile Organ safety profile Source Ligand Kd Non specific Reference human recombinant (CHO cells) [ 125 I]Tyr 11 -somatostatin-14 (0.1 nM) 1nM somatostatin-28 (1 µM) somatostatin-28 (IC 50 : 0.5 nM) Patel, C.Y. and Srikant, C.B. (1994) Endocrinology, 135: 2814-2817. Specialized cellular assays Standard profiles sst 1 cellul ar Ref. 2253 Ref. 2254 Q 3 weeks Agonist effect Antagonist effect Source human recombinant (CHO cells) Measured product cAMP Detection method HTRF Agonist effect Control somatostatin-28 (100 nM) Reference somatostatin-28 (EC 50 : 0.37 nM) Antagonist effect Stimulant somatostatin-28 (3 nM) Reference unavailable Patel, Y.C. and Srikant, C.B. (1994) Endocrinology, 135: 2814-2817. [Solvent] must be kept 0.3% Testing conditions Ordering information For further details and updated information on assays: ❚ Please go to www.cerep.com catalog online or contact us at sales@cerep.com ❚ Europe: +33 (0)5 49 89 30 00 – USA: +1 (425) 895 8666 – Japan: +81 (0)3 3354 4026 – China: +86 21 5132 0568 Assay developed in 2010 New assay conditions Human Q Standard turnaround time Assay list & index
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in vitro pharmacology 2011 catalog
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Cerep services p. 4 Receptors [GPC
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5 ❚ tool-box for cell-based assay
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7 ❚ profile design Cerep offers a
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9 ❚ data online A powerful web-ba
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11 in vitro pharmacology assays Rec
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13 Cerep services receptors Recept
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15 Adenosine ❚ A 2B - antagonist
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17 alpha 1B - antagonist radioligan
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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 and 48: melanin concentrating hormone ❚
Page 49 and 50: 49 ❚ melatonin Cerep services MT
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: 71 serotonin ❚ 5-HT 2B - agonist
Page 75 and 76: 75 ❚ thyrotropin releasing hormon
Page 77 and 78: 77 ❚ vasopressin Cerep services O
Page 79 and 80: 79 Cerep services receptors Recept
Page 81 and 82: 81 LXRb - agonist radioligand bindi
Page 83 and 84: 83 Cerep services receptors Recept
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
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123 TXK Ref. 2786 Q 3 weeks Include
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125 CDK6 (cycD3) Ref. 2909 Q 3 week
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protein-SERINE/THREONINE kinases [C
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129 JNK3 Ref. 2916 Q 3 weeks Includ
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131 CaMK1d Ref. 2922 Q 3 weeks Incl
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133 MAPKAPK2 Ref. 3367 Q 3 weeks I
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135 PhKg1 Ref. 2745 Q 3 weeks Inclu
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137 ❚ protein-SERINE/THREONINE ki
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139 MSK1 Ref. 1724 Q 3 weeks Source
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141 PKCe Ref. 2044 Q 3 weeks PKCz R
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143 ROCK2 Ref. 2884 Q 3 weeks Inclu
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145 COT kinase (MAP3K8) Ref. 2003 Q
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147 MKK6/p38a (mutant active) Ref.
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149 ❚ protein-SERINE/THREONINE ki
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151 RAF-1/MEK1 Ref. 1703 Q 3 weeks
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153 other kinases ❚ MYT1 kinase R
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155 other kinases ❚ TBK1 Ref. 33
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157 Cerep services Epigenetic & DNA
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159 HDACs ❚ HDAC3 Ref. 2083 Q 3 w
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161 HDACs ❚ sirtuin 3 Source Subs
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163 Cerep services Other enzymes Re
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165 phosphatases ❚ phosphatase LA
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167 phosphatase SHP2 (PTPN11) Sourc
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169 caspase-3 ❚ Cysteine protease
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171 proteases [aspartic proteases]
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173 proteases [metalloproteases]
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phosphodiesterases ❚ 175 PDE4A 1
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177 no synthases ❚ inducible NOS
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179 ❚ Monoamine & neurotransmitte
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181 Cerep services ❚ Transduction
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183 miscellaneous enzymes ❚ carbo
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185 Specialized cellular assays The
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187 ion transport systems ❚ Na +
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189 cytokine secretion ❚ IL-2 sec
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191 expression of endothelial adhes
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193 PDGF-stimulated Balb/c 3T3 prol
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195 cerep Standard profiles ExpresS
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197 ❚ Cellular functional GPCR pr
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Cerep standard profiles ❚ 199 Dr
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Cerep standard profiles ❚ 201 Sa
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203 testing conditions Binding, enz
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205 The reference compound for each
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207 ordering information Quotation
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209 REQUESTED COMPOUND INFORMATION
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shipment instructions ❚ 211 For
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213 assay list & index
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215 CDK5/p35 124 CDK6 (cycD3) 125 C
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217 MMP-3 172 MMP-7 172 MMP-8 172 M
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contacts ❚ france [Laboratories]
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