in vitro PHARMACOLOGY 2011 CATALOG - Cerep

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88 in vitro pharmacology 2011 catalog ❚ growth factors VEGF - agonist radioligand binding Ref. 0672 [Custom offer] Please contact us at: customresearch@cerep.com Source Ligand Kd Non specific Reference HUV-EC-C cells [ 125 I]VEGF (0.015 nM) 0.03 nM VEGF (3 nM) VEGF (IC 50 : 0.016 nM) Gitay-Goren, H. et al. (1996) J. Biol. Chem., 271: 5519-5523. β ❚ Imidazoline I 1 - agonist radioligand binding Ref. 0642 Q 3 weeks Included in: Diversity profile BioPrint ® profile Organ safety profile Source bovine adrenal medulla glands Ligand [ 3 H]clonidine (15 nM) (+ 10 µM RX 821002) Kd 16 nM Non specific rilmenidine (10 µM) Reference rilmenidine (IC 50 : 230 nM) Moldering, G.J. et al. (1993) Naun.-Sch. Arch. Pharm., 348: 70-76. specific binding (% of control) 100 50 0 -10 -9 -8 -7 -6 -5 log [drug] (M) rilmenidine I 2 - antagonist radioligand binding Ref. 0081 Q 3 weeks Included in: Diversity profile Organ safety profile Source Ligand Kd Non specific Reference rat cerebral cortex [ 3 H]idazoxan (2 nM) (+ 1 µM yohimbine) 4 nM cirazoline (10 µM) idazoxan (IC 50 : 8.4 nM) Brown, C.M. et al. (1990) Brit. J. Pharmacol., 99: 803-809. specific binding (% of control) 100 50 0 -11 -10 -9 -8 -7 -6 -5 -4 log [drug] (M) idaxoxan guanabenz clonidine phentolamine ❚ Insulin insulin - agonist radioligand binding Ref. 0084 [Custom offer] Please contact us at: customresearch@cerep.com Source Ligand Kd Non specific Reference rat liver [ 125 I]insulin (0.03 nM) 8 nM insulin (10 µM) insulin (IC 50 : 17 nM) Koch, R. and Weber, U. (1981) Hoppe-Seyler’s Z. Physiol. Chem., 362: 347-351. specific binding (% of control) 100 50 0 -10 -9 -8 -7 -6 log [drug] (M) insulin glucagon
89 ❚ Melatonin MT 3 (ML 2 ) - agonist radioligand binding Ref. 0088 Q 3 weeks Included in: BioPrint ® profile Organ safety profile Source Ligand Kd Non specific Reference hamster brain [ 125 I]2-iodomelatonin (0.1 nM) 4.8 nM melatonin (30 µM) melatonin (IC 50 : 96.5 nM) Pichering, D.S. and Niles, L.P. (1990) Eur. J. Pharmacol., 175: 71-77. ❚ See other Melatonin assays, page 49 Cerep services Receptors [Other receptors] Ion channels ❚ Nicotinic Transporters 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 Kinases Epigenetic & DNA-related enzymes Other enzymes Specialized cellular assays 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) Standard profiles Testing conditions 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 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.
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 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: 87 glycine (strychnine-insensitive)
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
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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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