in vitro PHARMACOLOGY 2011 CATALOG - Cerep

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100 in vitro pharmacology 2011 catalog ❚ nicotinic channels N muscle-type - antagonist radioligand binding Ref. 0936 Q 3 weeks Included in: BioPrint ® profile Source Ligand Kd Non specific Reference TE671 cells (endogenous) N neuronal (a4b2) - agonist radioligand binding Ref. 3029 Q 3 weeks Included in: Diversity profile BioPrint ® profile Organ safety profile [ 125 I]α-bungarotoxin (0.5 nM) 9.5 nM α-bungarotoxin (5 µM) α-bungarotoxin (IC 50 : 14 nM) specific binding (% of control) 100 50 0 -10 -9 -8 -7 -6 -5 -4 log [drug] (M) α-bungarotoxin tubocurarine nicotine atropine Lukas, R.J. (1986) J. Neurochem., 46: 1936-1941. [Custom offer] mouse BC3H1 cells model (Ref. 0111), please contact us at customresearch@cerep.com Source Ligand Kd (nM) Non specific Reference SH-SY5Y cells (endogenous) [ 3 H]cytisine (0.6 nM) 0.3 nM nicotine (10 µM) nicotine bitartrate salt (IC 50 : 3 nM) Gopalakrishnan et al.(1996) J. Pharmacol. Exp. Ther., 276: 289-297. α N neuronal (a4b2) - agonist radioligand binding Ref. 0110 [Custom offer] Please contact us at: customresearch@cerep.com Source Ligand Kd Non specific Reference rat cerebral cortex [ 3 H]cytisine (1.5 nM) 1.8 nM nicotine (10 µM) nicotine (IC 50 : 8.7 nM) Pabreza, L.A. et al. (1991) Mol. Pharmacol., 39: 9-12. specific binding (% of control) 100 50 nicotine carbachol atropine 0 α-bungarotoxin -10 -8 -7 -6 -5 -4 -9 -3 log [drug] (M) N neuronal (a7) - antagonist radioligand binding Ref. 0567 [Custom offer] Please contact us at: customresearch@cerep.com Source Ligand Kd Non specific Reference rat cerebral cortex [ 125 I]α-bungarotoxin (1 nM) 0.3 nM α-bungarotoxin (1 µM) α-bungarotoxin (IC 50 : 1.7 nM) Sharples, C.G.V. et al. (2000) J. Neurosci., 20: 2783-2791. specific binding (% of control) 100 50 0 -10 -9 -7 -6 -5 -4 -3 -11 -8 log [drug] (M) α-bungarotoxin epibatidine tubocurarine nicotine N neuronal (a7) - antagonist radioligand Source SH-SY5Y cells (endogenous) Ligand [ 125 I]α-bungarotoxin binding Kd (nM) 0.34 nM Ref. 3010 Non specific α-bungarotoxin (1 µM) Q 3 weeks Reference α-bungarotoxin (IC 50 : 2.1 nM) Included in: Organ safety profile Sharples et al.(2000) J. Neurosci., 20: 2783-2791. α 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
101 ❚ purinergic channels Cerep services P2X - agonist radioligand binding Ref. 0127 Q 3 weeks Included in: High-throughput profile Diversity profile Organ safety profile Source Ligand Kd Non specific Reference rat urinary bladder [ 3 H]α,β-MeATP (3 nM) 2.6 nM α,β-MeATP (10 µM) α,β-MeATP (IC 50 : 3.5 nM) Bo, X. and Burnstock, G. (1990) Brit. J. Pharmacol., 101: 291-296. specific binding (% of control) 100 50 0 -10 -9 -8 -7 -6 -5 -4 -3 log [drug] (M) α,β-MeATP suramin adenosine Receptors Ion channels P2X tissue Ref. 0332 Q 4 weeks Source rabbit ear artery (endothelium-denuded) Agonist α,βMeATP (pD 2 = 6.9) Antagonist suramin (pA 2 = 4.9) Test concentrations 3 concentrations, n=2 (2 tissues) for both activities [Solvent] must be kept ≤ 0.1% O’Connor, S.E. et al. (1990) Brit. J. Pharmacol., 101: 640-644. ❚ serotonin channels 5-HT 3 - antagonist radioligand binding Ref. 0411 Q 3 weeks Included in: ExpresS Profile High-throughput profile BioPrint ® profile Organ safety profile 5-HT 3 tissue Ref. 0335 Q 4 weeks Source Ligand Kd Non specific Reference human recombinant (CHO cells) [ 3 H]BRL 43694 (0.5 nM) 1.15 nM MDL 72222 (10 µM) MDL 72222 (IC 50 : 10 nM) Hope, A.G. et al. (1996) Brit. J. Pharmacol., 118: 1237-1245. Source selected cerep assays guinea-pig colon Agonist serotonin (pD 2 = 5.6) Antagonist MDL 72222 (pA 2 = 5.7) Test concentrations 3 concentrations, n=2 (2 tissues) for both activities [Solvent] must be kept ≤ 0.1% Butler, A. et al. (1990) Brit. J. Pharmacol., 101: 591-598. tension (% of max.) 100 50 0 -9 -8 -7 -6 -5 -4 log [agonist] (M) suramin none 30 µM 100 µM 300 µM ❚ See other Purinergic assays, pp.67 and 90 specific binding (% of control) tension (% of max.) 100 50 0 100 50 0 -11 -10 -9 -8 -7 -6 -5 -4 -3 log [drug] (M) -8 -7 -6 -5 -4 log [agonist] (M) MDL 72222 serotonin 8-OH-DPAT ketanserin MDL 72222 none 1 µM 3 µM 10 µM ❚ See other Serotonin assays, pp. 69, 90 and 105 ❚ binding assays Binding assays are developed according to the competition assay principle. There are three assay formats used: filtration, scintillation proximity assay (SPA) and centrifugation. All formats utilize a radiolabeled ligand and a source of receptor (membranes, soluble/purified). Large batches of cells, from which prepared membranes are frozen and stored, are produced in-house. Membrane preparations are quality controlled before use. ❚ tissue bioassays Tissue bioassays are functional assays designed to evaluate the agonist and antagonist activities of compounds at various receptors and ion channels in whole tissues. The tissues used are isolated from contractile cardiac and smooth muscles of the cardiovascular, respiratory, gastrointestinal and urogenital tracts of rodents, rabbit or human. The selected tissues are assayed in organ bath systems to record the contractile activity in conditions as selective as possible to avoid any potential interaction with other receptors known to be present in the tissue used. Transporters Kinases Epigenetic & DNA-related enzymes Other enzymes Specialized cellular assays Standard profiles Testing conditions Ordering information 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
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adrenergic ❚ 21 beta 3 cellul ar
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-12 -11 -10 -9 -8 -7 -6 -5 -4 -3 bo
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adykinin ❚ 25 B 2 cellul ar Ref.
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27 ❚ cannabinoid CB 1 - agonist r
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29 chemokines ❚ CCR2 cellul ar Re
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31 cholecystokinin ❚ CCK 2 (CCK B
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33 dopamine ❚ D 2S - antagonist r
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dopamine ❚ 35 D 5 cellul ar Ref.
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37 Cerep services ❚ Free fatty ac
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39 galanin ❚ GAL 2 - agonist radi
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41 ❚ Growth hormone-releasing hor
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43 H 3 - agonist radioligand Source
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45 leukotrienes ❚ CysLT 2 (LTC 4
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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 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 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: 99 kainate - agonist radioligand bi
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
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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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