in vitro PHARMACOLOGY 2011 CATALOG - Cerep

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60 in vitro pharmacology 2011 catalog ❚ opioid and opioid-like kappa (KOP) cellul ar Ref. 2071 Ref. 2072 Q 3 weeks Included in: Agonist effect Antagonist effect Cellular functional GPCR profile Source rat recombinant (CHO cells) Measured product cAMP Detection method HTRF Agonist effect Control U 50488 (1 µM) Reference U 50488 (EC 50 : 1.1 nM) Antagonist effect Stimulant U 50488 (100 nM) Reference nor-BNI (IC 50 : 9.2 nM) Avidor-Reiss, T. et al. (1995) FEBS Lett., 361: 70-74. cAMP modulation (% of control) 100 50 0 -12 -11 -10 -9 -8 -7 -6 -5 -4 -11 -10 -9 -8 -7 -6 -5 log [agonist] (M) U 50488 U 69593 DAMGO DPDPE 100 50 0 log [antagonist] (M) nor-BNI naloxone naltrexone DGNTI kappa (KOP) tissue Ref. 0329 Q 4 weeks Source rabbit vas deferens (field-stimulated) Agonist U 69593 (pD 2 = 7.8) Antagonist nor-BNI (pA 2 = 10.8) Test concentrations 3 concentrations, n=2 (2 tissues) for both activities [Solvent] must be kept ≤ 0.1% Oka, T. et al. (1980) Eur. J. Pharmacol., 73: 235-236. tension (% of control) -12 -11 -12 -11 -11 -10 100-12 -11 -9 -8 -7 -6 -5 -4 -10 -9 -8 -7 -10 -9 -8 -7 50 -10 -9 -8 -7 -6 -5 -9 -8 -7 -6 -5 -10 -4 0 -11 -10 -9 -8 -7 -6 -5 -4 -13 -12 -11 -10 -9 -8 -7 -6 -10 -9 -8 -7 -6 log [agonist] (M) -12 -11 -10 -9 -8 -7 -6 -5 -4 nor-BNI none 0.1 nM 0.3 nM 1 nM mu (MOP) - antagonist radioligand Source human recombinant (HEK-293 cells) Ligand [ 3 H]diprenorphine (0.4 nM) Kd 0.14 nM Non specific naltrexone (1 µM) binding Reference naltrexone (IC 50 : 1.1 nM) Ref. 1666 Q 3 weeks Zhang, S. et al. (1998) J. Pharmacol. Exp. Ther., 286: 136-141. specific binding (% of control) 100 50 0 -11 -10 -9 -8 -7 -6 -5 -4 log [drug] (M) naltrexone DAMGO U 50488 DPDPE mu (MOP) - agonist radioligand binding Ref. 0118 Q 3 weeks Included in: ExpresS Profile High-throughput profile BioPrint ® profile Organ safety profile mu (MOP) cellul ar Ref. 1392 Ref. 1393 Q 3 weeks Included in: Agonist effect Antagonist effect Cellular functional GPCR profile Source Ligand Kd Non specific Reference human recombinant (HEK-293 cells) [ 3 H]DAMGO (0.5 nM) 0.35 nM naloxone (10 µM) DAMGO (IC 50 : 0.537 nM) specific binding (% of control) 100 50 0 -11 -10 -9 -8 -7 -6 -5 log [drug] (M) Wang, J.-B. et al. (1994) FEBS Lett., 338: 217-222. [Custom offer] rat brain model (Ref. 0117), please contact us at customresearch@cerep.com Source human recombinant (CHO cells) Measured product cAMP Detection method HTRF Agonist effect Control DAMGO (1 µM) Reference DAMGO (EC 50 : 2.8 nM) Antagonist effect Stimulant DAMGO (30 nM) Reference CTOP (IC 50 : 335 nM) Wang, J.B. et al. (1994) FEBS Lett., 338: 217-222. cAMP modulation (% of control) 100 50 0 log [agonist] (M) DAMGO DPDPE fentanyl morphine 100 [Solvent] must be kept ≤ 0.3% DAMGO naloxone U 50488 DPDPE -12 -11 -10 -9 -8 -7 -6 -5 -10 -9 -8 -7 -6 -5 50 0 log [antagonist] (M) CTOP naltrexone naltrindole naloxone mu (MOP) tissue Ref. 0330 Q 4 weeks Source guinea-pig ileum (field-stimulated) Agonist DAMGO (pD 2 = 8.3) Antagonist naloxone (pA 2 = 8.8) Test concentrations 3 concentrations, n=2 (2 tissues) for both activities [Solvent] must be kept ≤ 0.1% Hutchinson, M. et al. (1975) Brit. J. Pharmacol., 55: 541-546. tension (% of control) -12 -11 -12 -11 -11 -10 100-12 -11 -9 -8 -7 -6 -5 -4 -10 -9 -8 -7 -10 -9 -8 -7 50 -10 -9 -8 -7 -6 -5 -9 -8 -7 -6 -5 -10 -4 0 -11 -10 -9 -8 -7 -6 -5 -4 -13 -12 -11 -10 -9 -8 -7 -6 log [agonist] (M) -12 -11 -10 -9 -8 -7 -6 -5 -4 -10 -9 -8 -7 -6 naloxone none 3 nM 10 nM 30 nM
61 NOP (ORL1) - agonist radioligand binding Ref. 0358 Q 3 weeks Included in: ExpresS Profile High-throughput profile Diversity profile BioPrint ® profile Organ safety profile Source Ligand Kd Non specific Reference human recombinant (HEK-293 cells) [ 3 H]nociceptin (0.2 nM) 0.4 nM nociceptin (1 µM) nociceptin (IC 50 : 1.1 nM) Ardati, A. et al. (1997) Mol. Pharmacol., 51: 816-824. specific binding (% of control) opioid and opioid-like ❚ 100 50 nociceptin DAMGO 0 DPDPE U 50488 -12 -11 -10 -9 -8 -7 -6 -5 log [drug] (M) Cerep services Receptors [GPCRs] NOP (ORL1) cellul ar Ref. 2381 Agonist effect Ref. 2382 Antagonist effect Q 3 weeks Source human recombinant (CHO cells) Measured product cAMP Detection method HTRF Agonist effect Control nociceptin (10 nM) Reference nociceptin (EC 50 : 0.1 nM) Antagonist effect Stimulant nociceptin (1 nM) Reference UFP-101 (IC 50 : 64 nM) New, D.C. and Wong, Y.H. (2002) Neurosign., 11: 197-212. [Solvent] must be kept 0.3% Ion channels Transporters NOP (ORL1) tissue Ref. 1226 Q 4 weeks Source mouse vas deferens (field-stimulated) Agonist nociceptin (pD 2 = 7.9) Antagonist UFP-101 Test concentrations 3 concentrations, n=2 (2 tissues) for both activities [Solvent] must be kept ≤ 0.1% Calo, G. et al. (2002) Brit. J. Pharmacol., 136: 303-311. tension (% of control) 100 50 0 log [agonist] (M) -11 -10 -9 -8 -7 -6 Kinases Epigenetic & DNA-related enzymes ❚ Orexin Other enzymes OX 1 - agonist radioligand Source human recombinant (CHO cells) Ligand [ 125 I]orexin-A (0.1 nM) binding Kd 10 nM Ref. 1987 Non specific SB 334867 (1 µM) Q 3 weeks Reference orexin-A (IC 50 : 0.49 nM) Included in: Organ safety profile Langmead, C.J. et al. (2004) Brit. J. Pharmacol., 141: 340-346. Specialized cellular assays Standard profiles OX 1 cellul ar Ref. 2234 Ref. 2235 Q 3 weeks Agonist effect Antagonist effect Source human recombinant (CHO cells) Measured product intracellular [Ca 2+ ] Detection method fluorimetry Agonist effect Control orexin-A (10 nM) Reference orexin-A (EC 50 : 0.8 nM) Antagonist effect Stimulant orexin-A (3 nM) Reference SB 334867 (IC 50 : 210 nM) Smart, D. et al. (2001) Brit. J. Pharmacol., 132: 1179-1182. Ca 2+ mobilization (% of control) 100 100 50 50 0 0 -9 -8 -7 -6 -8 -11 -10 -7 -6 -5 log [agonist] (M) log [antagonist] (M) orexin-A SB 334867 orexin-B SB 408124 [Ala 11 ,D-Leu 15 ]-orexin-B [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 -12 -11 -11 -10 -9 -8 -7 -6 -5 -4 -12 -11 -10 -9 -8 -7 ❚ 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 -10 -9 -8 -7 -6 -5 -9 -8 -7 -6 -5 -10 -4 -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
Page 9 and 10: 9 ❚ data online A powerful web-ba
Page 11 and 12: 11 in vitro pharmacology assays Rec
Page 13 and 14: 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: 59 Cerep services ❚ opioid and op
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 81 and 82: 81 LXRb - agonist radioligand bindi
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
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111 protein-tyrosine kinases [Rtk]
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113 FLT-3 kinase Ref. 2866 Q 3 week
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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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