in vitro PHARMACOLOGY 2011 CATALOG - Cerep

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66 in vitro pharmacology 2011 catalog ❚ prostanoid TP (TXA 2 /PGH 2 ) - antagonist radioligand binding Ref. 2048 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]SQ 29548 (5 nM) 4 nM U 44069 (10 µM) U 44069 (IC 50 : 12 nM) Abramovitz, M. et al. (2000) Biochem. Biophys. Acta., 1483: 285-293. specific binding (% of control) 100 50 0 -12 -11 -10 -9 -8 -7 -6 -5 -4 -3 log [drug] (M) U 44069 U 46619 PGF2α PGE2 TP (TXA 2 /PGH 2 ) cellul ar Ref. 2059 Agonist effect Ref. 2060 Antagonist effect Q 3 weeks Source human recombinant (HEK-293 cells) Measured product intracellular [Ca 2+ ] Detection method fluorimetry Agonist effect Control U 44069 (1 µM) Reference U 44069 (EC 50 : 5 nM) Antagonist effect Stimulant U 44069 (30 nM) Reference L 670596 (IC 50 : 25 nM) Elmhurst, J.L. et al. (1997) J. Pharmacol. Exp. Ther., 283: 1198-1205. Ca 2+ mobilization (% of control) 100 50 0 -11 -10 -9 -8 -7 -6 -5 -4 -10 -9 -8 -7 -6 -5 log [agonist] (M) U 44069 U 46619 PGE2 PGF2α 100 [Solvent] must be kept ≤ 0.1% 50 0 log [antagonist] (M) L 670596 SQ 29548 AL 8810 AH 6809 -11 -10 -9 -8 -7 -6 -5 -4 -12 -11 -10 -9 -8 -7 -11 -10 -9 -8 -7 -6 -5 -4 -12 -11 -10 -9 -8 -7 -12 -11 -10 -9 -8 -7 -6 -5 -9 -8 -7 -6 -5 -10 -4 ❚ proteinase-activated PAR1 - agonist radioligand binding Ref. 2592 Q 3 weeks Included in: Diversity profile Source Ligand Kd Non specific Reference human recombinant (KNRK cells) [ 3 H]ha-TRAP (0.5 nM) 0.25 nM ha-TRAP (10 µM) ha-TRAP (IC 50 : 1.3 nM) Ahn, H.S. et al. (1997) Mol. Pharmacol., 51: 350-356. PAR1 cellul ar Ref. 2332 Ref. 2333 Q 3 weeks Agonist effect Antagonist effect Source human recombinant (KNRK cells) Measured product intracellular [Ca 2+ ] Detection method fluorimetry Agonist effect Control TFLLR-NH 2 (100 µM) Reference TFLLR-NH 2 (EC 50 : 3.6 µM) Antagonist effect Stimulant TFLLR-NH 2 (10 µM) Reference SCH 79797 (IC 50 : 935 nM) Kawabata, A. et al. (1999) J. Pharmacol. Exp. Ther., 288: 358-370. Ca 2+ mobilization (% of control) 100 100 50 50 0 0 -10 -9 -8 -7 -6 -5 -4 -9 -8 -7 -6 -5 -12 -11 -4 log [agonist] (M) log [antagonist] (M) TFLLR-NH 2 SCH 79797 SLIGRL-NH 2 FSLLRY-NH 2 thrombin 3-mercaptopropionyl-F-Cha- trypsin Cha-RKPBDK-NH 2 tcY-NH 2 [Solvent] must be kept ≤ 0.1% PAR2 - agonist radioligand Source human recombinant (Hela cells) Ligand [ 3 H]2-fuoryl-LIGRL-NH 2 (2.5 nM) binding Kd 13 nM Ref. 2424 Non specific 2-fuoryl-LIGRL-NH 2 (10 µM) Q 3 weeks Reference SLIGRL-NH 2 (IC 50 : 67 nM) Included in: Organ safety profile Kanke, T. et al. (2005) Brit. J. Pharmacol., 145: 255-263. -12 -11 -12 -11 -11 -10 -12 -11 -7 -6 -5 -9 -8 -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
67 proteinase-activated ❚ PAR2 cellul ar Ref. 2323 Ref. 2324 Q 3 weeks Agonist effect Antagonist effect Source human recombinant (Hela cells) Measured product intracellular [Ca 2+ ] Detection method fluorimetry Agonist effect Control trypsin (100 µM) Reference trypsin (EC 50 : 169 nM) Antagonist effect Stimulant trypsin (1 µM) Reference unavailable Kawabata, A. et al. (1999) J. Pharmacol. Exp. Ther., 288: 358-370. [Solvent] must be kept 0.1% Cerep services Receptors [GPCRs] ❚ purinergic Ion channels P2Y - agonist radioligand binding Ref. 0128 Q 3 weeks Included in: High-throughput profile Diversity profile Organ safety profile Source Ligand Kd Non specific Reference rat cerebral cortex [ 35 S]dATPαS (10 nM) 10 nM dATPαS (10 µM) dATPαS (IC 50 : 20 nM) Simon, J. et al. (1995) Pharmacol. Toxicol., 76: 302-307. specific binding (% of control) 100 50 0 -10 -9 -8 -7 -6 -5 -4 log [drug] (M) dATPαS ADPβS suramin α,β-MeATP Transporters Kinases P2Y 1 cellul ar Ref. 2132 Ref. 2134 Q 3 weeks Agonist effect Antagonist effect Source human recombinant (1321N1 cells) Measured product intracellular [Ca 2+ ] Detection method fluorimetry Agonist effect Control MRS 2365 (100 nM) Reference MRS 2365 (EC 50 : 0.24 nM) Antagonist effect Stimulant MRS 2365 (1 nM) Reference MRS 2500 (IC 50 : 39.3 nM) Chhatriwala, M. et al. (2004) J. Pharmacol. Exp. Ther., 311: 1038-1043. [Solvent] must be kept 0.1% Epigenetic & DNA-related enzymes Other enzymes P2Y 2 cellul ar Ref. 2164 Ref. 2167 Q 3 weeks Agonist effect Antagonist effect Source human recombinant (1321N1 cells) Measured product intracellular [Ca 2+ ] Detection method fluorimetry Agonist effect Control UTP (3 µM) Reference UTP (EC 50 : 60 nM) Antagonist effect Stimulant UTP (300 nM) Reference unavailable Kassack, M.U. et al. (2002) J. Biomol. Screen., 7: 233-246. Ca 2+ mobilization (% of control) 100 50 0 -9 -8 -7 -6 -5 -10 -4 log [agonist] (M) UTP UDP MRS 2365 2MeSADP [Solvent] must be kept ≤ 0.1% antagonist effect: no graph available Specialized cellular assays Standard profiles P2Y 4 cellul ar Ref. 2165 Ref. 2168 Q 3 weeks Agonist effect Antagonist effect Source human recombinant (1321N1 cells) Measured product intracellular [Ca 2+ ] Detection method fluorimetry Agonist effect Control UTP (100 nM) Reference UTP (EC 50 : 1.9 nM) Antagonist effect Stimulant UTP (10 nM) Reference unavailable Herold, C.L. et al. (2004) J. Biol. Chem., 279: 11456-11464. Ca 2+ mobilization (% of control) -12 -11 -12 -11 100 -12 -11 50 -10 -9 -8 -7 -10 -9 -8 -7 -6 -5 0 -11 -10 -9 -8-12 -7 -11 -10 -6 -9-5 -10 -8-4-7 -6 -5 -4 -9 -8 -7 -6 -5 -4 -12 -11 -10 -9 -8 -7 -6 -5 -4 -3 antagonist effect: -10 -9 -8 -7 no graph available log [agonist] (M) UTP UDP MRS 2365 2MeSADP [Solvent] must be kept ≤ 0.1% Testing conditions Ordering information -11 -10 -9 -8 -7 -6 -5 -4 For further details and updated information on assays: ❚ Please go to www.cerep.com catalog online or contact us at sales@cerep.com -12 -11 -11 -10 -12 -11 -9 -8 -7 -6 -5 -4 -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 -12 -11 -10 -9 -8 -7 -6 -5 -4 -3 ❚ Europe: +33 (0)5 49 89 30 00 – USA: +1 (425) 895 8666 – Japan: +81 (0)3 3354 4026 – China: -12 -11+86 -10 -921 -8 5132 -7 0568 Assay developed in 2010 New assay conditions Human Q Standard turnaround time -12 -11 -10 -9 -8 -7 -6 -5 -4 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
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 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: 65 prostanoid ❚ EP 4 - agonist ra
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 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
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117 TRKB Ref. 2902 Q 3 weeks Includ
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119 protein-tyrosine kinases [Ctk]
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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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