in vitro PHARMACOLOGY 2011 CATALOG - Cerep

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162 in vitro pharmacology 2011 catalog ❚ notes ❚ see also ADME-Tox & PK 2011 catalog ADME-Tox & PK 2011 CATALOG IN VITRO ADME Solution properties Drug absorption/drug transport Drug metabolism Drug-drug interactions IN VITRO TOXICITY Cardiac toxicity Cytotoxicity Genetic toxicity IN VIVO PK/BIOANALYTICAL In vivo PK Bioanalytical ASSAY SELECTION GUIDE STANDARD PROFILES APPLICATION NOTES
163 Cerep services Other enzymes Receptors Ion channels ❚ Phosphatases Transporters Reversibility of protein tyrosine residue phosphorylation is an important factor in the intra-cellular signalling as phosphorylation induces conformational changes, creates docking sites for other proteins and causes intracellular relocation. This reversibility relies on the co-ordinated actions of protein tyrosine kinases and protein tyrosine phosphatases (PTPs). Protein tyrosine phosphatases are divided in receptor PTPs (rPTPs) and non receptor PTPs (nrPTPs), the dual specificity PTP (dsPTPs) and the low molecular PTP families. They are involved in cell-substrate adhesion, cell-cell adhesion and insulin signalling as described in Protein tyrosine phospshatase end signaling, Stoker, A.S. (2005), J. Endocrinol., 185: 19-33. In this context, Cerep has designed a high throughput profiling platform to determine the inhibitory activity of compounds on the phosphates superfamily. The robustness, reproducibility and relevance of this platform were determined by screening a panel of commercially available reference inhibitors in three independent experiments. Kinases Epigenetic & DNA-related enzymes phosphatase PP1a Ref. 2656 Q 3 weeks Source human recombinant (E. coli) Substrate DIFMUP (250 µM) Measured product DIFMU Detection method fluorimetry Reference LR-microcystin (IC 50 : 9 nM) Honkanen, R.E. et al. (1990) J. Biol. Chem., 265: 19401-19404. Other enzymes Specialized cellular assays phosphatase 1B (PTP1B) Ref. 2593 Q 3 weeks Included in: Non-kinase enzyme profile Diversity profile Organ safety profile Source Substrate Measured product Detection method Reference human recombinant (E. coli) DIFMUP (100 µM) DIFMU fluorimetry Welte, S. et al. (2005) Anal. Biochem., 338: 32-38. ammonium molybdate (IC 50 : 420 nM) Standard profiles Testing conditions phosphatase 2A (PP2A) Source human recombinant Substrate DIFMUP (100 µM) Measured product DIFMU Detection method fluorimetry Ref. 2584 Reference LR-microcystin (IC 50 : 8.7 nM) Q 3 weeks Fontal, O.I. et al. (1999) Anal. Bioch., 269: 289-296. 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 ❚
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49 ❚ melatonin Cerep services MT
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51 M 2 - antagonist radioligand bin
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53 muscarinic ❚ M 5 - antagonist
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55 NK 3 - agonist radioligand bindi
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neuropeptide y ❚ 57 Y 1 cellul a
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59 Cerep services ❚ opioid and op
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61 NOP (ORL1) - agonist radioligand
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63 platelet activating factor ❚ P
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65 prostanoid ❚ EP 4 - agonist ra
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67 proteinase-activated ❚ PAR2 ce
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serotonin ❚ 69 5-HT 1A cellul ar
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71 serotonin ❚ 5-HT 2B - agonist
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73 5-HT 7 - agonist radioligand bin
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75 ❚ thyrotropin releasing hormon
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77 ❚ vasopressin Cerep services O
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81 LXRb - agonist radioligand bindi
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85 gaba ❚ GABA A1 (a1, b2, g2) -
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87 glycine (strychnine-insensitive)
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89 ❚ Melatonin MT 3 (ML 2 ) - ago
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91 ❚ Sigma Cerep services sigma (
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93 Cerep services [Voltage-gated ch
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voltage-gated channels [K + channel
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transient receptor potential channe
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99 kainate - agonist radioligand bi
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101 ❚ purinergic channels Cerep s
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103 Cerep services transporters Rec
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105 norepinephrine ❚ norepinephri
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107 Cerep services Kinases Receptor
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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: 161 HDACs ❚ sirtuin 3 Source Subs
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
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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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in vitro PHARMACOLOGY 2011 CATALOG - Cerep

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