in vitro PHARMACOLOGY 2011 CATALOG - Cerep

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64 in vitro pharmacology 2011 catalog ❚ prostanoid EP 1 - agonist radioligand Source human recombinant (HEK-293 cells) Ligand [ 3 H]PGE 2 (1.5 nM) Kd 1.5 nM Non specific PGE 2 (10 µM) binding Reference PGE 2 (IC 50 : 1.4 nM) Ref. 0440 Q 3 weeks Sharif, N.A. and Davis, T.L. (2002) J. Pharm. Pharmacol., 54: 539-547. specific binding (% of control) 100 50 0 -12 -11 -10 -9 -8 -7 -6 -5 -4 log [drug] (M) PGE2 AH 6809 butaprost AH 23848 EP 1 cellul ar Ref. 2053 Ref. 2054 Q 3 weeks Agonist effect Antagonist effect Source human recombinant (HEK-293 cells) Measured product intracellular [Ca 2+ ] Detection method fluorimetry Agonist effect Control PGE 2 (100 nM) Reference PGE 2 (EC 50 : 0.88 nM) Antagonist effect Stimulant PGE 2 (3 nM) Reference SC 51322 (IC 50 : 53.7 nM) Ungrin, M.D. et al. (1999) Analytical Biochem., 272: 34-42. Ca 2+ mobilization (% of control) 100 50 0 -12 -11 -10 -9 -8 -7 -6 -5 -4 log [agonist] (M) PGE2 17-phenyl PGE2 PGF2α U 44069 100 [Solvent] must be kept ≤ 0.1% 50 0 -9 -8 -7 -6 -5 log [antagonist] (M) SC 51322 AL 8810 AH 23848 AH 6809 EP 2 - agonist radioligand binding Ref. 1955 Q 3 weeks Included in: High-throughput profile Diversity profile BioPrint ® profile Organ safety profile Source Ligand Kd Non specific Reference human recombinant (HEK-293 cells) [ 3 H]PGE 2 (3 nM) 3 nM PGE 2 (10 µM) PGE 2 (IC 50 : 1.7 nM) Abramovitz, M. et al. (2000) Biochem. Biophys. Acta., 1483: 285-293. -12 -11 -12 -11 -11 -10 -12 -11 -9 -8 -7 -6 -5 -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 EP 2 cellul ar Ref. 1956 Ref. 1957 Q 3 weeks Agonist effect Antagonist effect Source human recombinant (CHO cells) Measured product cAMP Detection method HTRF Agonist effect Control PGE 2 (10 µM) Reference PGE 2 (EC 50 : 100 nM) Antagonist effect Stimulant PGE 2 (300 nM) Reference AH 6809 (IC 50 : 3.9 µM) Wilson, R.J. et al. (2004) Eur. J. Pharmacol., 501: 49-58. cAMP modulation (% of control) 100 100 50 50 0 0 -9 -8 -7 -6 -5 -8 -7 -6 -5 -4 log [agonist] (M) log [antagonist] (M) PGE2 AH 6809 butaprost AH 23848 AH 13205 U 44069 [Solvent] must be kept ≤ 0.3% EP 3 - agonist radioligand Source human recombinant (HEK-293 cells) Ligand [ 3 H]PGE 2 (0.5 nM) Kd 0.8 nM Non specific PGE 2 (1 µM) binding Reference sulprostone (IC 50 : 2.9 nM) Ref. 2774 Q 3 weeks Abramovitz, M. et al. (2000) Biochem. Biophys. Acta., 1483: 285-293. -12 -11 -10 -9 -8 -7 -6 -5 -9 -8 -7 -6 -5 -10 -4 EP 3 cellul ar Ref. 2577 Ref. 2578 Q 3 weeks Agonist effect Antagonist effect Source human recombinant (HEK-293 cells) Measured product impedance Detection method cellular dielectric spectroscopy Agonist effect Control sulprostone (10 nM) Reference sulprostone (EC 50 : 0.058 nM) Antagonist effect Stimulant sulprostone (0.1 nM) Reference unavailable Asboth, G. et al. (1996) Endocrinol., 137: 2572-2579. [Solvent] must be kept 0.1%
65 prostanoid ❚ EP 4 - agonist radioligand Source human recombinant (HEK-293 cells) Ligand [ 3 H]PGE 2 (0.5 nM) Kd 0.3 nM Non specific PGE 2 (10 µM) binding Reference PGE 2 (IC 50 : 1.9 nM) Ref. 0441 Q 3 weeks Abramovitz, M. et al. (2000) Biochem. Biophys. Acta., 1483: 285-293. α Cerep services Receptors [GPCRs] EP 4 cellul ar Ref. 1871 Ref. 1872 Q 3 weeks Agonist effect Antagonist effect Source human recombinant (CHO cells) Measured product cAMP Detection method HTRF Agonist effect Control PGE 2 (1 µM) Reference PGE 2 (EC 50 : 7.1 nM) Antagonist effect Stimulant PGE 2 (30 nM) Reference unavailable Wilson, R.J. et al. (2004) Eur. J. Pharmacol., 501: 49-58. cAMP modulation (% of control) 100 50 0 -12 -11 -10 -9 -8 -7 -6 -5 log [agonist] (M) PGE2 thromboxane 17-phenyl PGE2 [Solvent] must be kept ≤ 0.3% -4 antagonist effect: no graph available Ion channels Transporters FP - agonist radioligand binding Ref. 1979 Q 3 weeks Included in: BioPrint ® profile Source Ligand Kd Non specific Reference human recombinant (HEK-293 cells) [ 3 H]PGF 2a (2 nM) 3.83 nM cloprostenol (10 µM) PGF 2a (IC 50 : 2.02 nM) Abramovitz, M. et al. (2000) Biochem. Biophys. Acta., 1483: 285-293. specific binding (% of control) 100 50 -9 -8 -7 -6 -5 -10 -4 0 -12 -11 -10 -9 -8 -7 -6 -5 -4 log [drug] (M) PGF2α cloprostenol latanoprost AH 23848 Kinases Epigenetic & DNA-related enzymes FP cellul ar Ref. 2011 Ref. 2013 Q 3 weeks Agonist effect Antagonist effect Source human recombinant (HEK-293 cells) Measured product intracellular [Ca 2+ ] Detection method fluorimetry Agonist effect Control PGF 2a (1 µM) Reference PGE 2a (EC 50 : 1.9 nM) Antagonist effect Stimulant PGF 2a (10 nM) Reference unavailable Sharif, N.A. et al. (2003) Prost. Leuk. Ess. Fatty Acids, 68: 27-33. Ca 2+ mobilization (% of control) 100 50 0 -11 -10 log [agonist] (M) PGF2α cloprostenol latanoprost PGE2 -9 -8 -7 -6 [Solvent] must be kept ≤ 0.1% antagonist effect: no graph available Other enzymes Specialized cellular assays IP (PGI 2 ) - agonist radioligand binding Ref. 2230 Q 3 weeks Included in: High-throughput profile Diversity profile BioPrint ® profile Organ safety profile Source Ligand Kd Non specific Reference human recombinant (HEK-293 cells) [ 3 H]iloprost (10 nM) 8 nM iloprost (10 µM) iloprost (IC 50 : 22 nM) Abramovitz, M. et al. (2000) Biochem. Biophys. Acta., 1483: 285-293. specific binding (% 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 -12 -11 -10 -9 -8 -7 -6 -5 -4 -3 -12 -11 -10 -9 -8 -7 -6 -5 log [drug] (M) iloprost PGF2α U 46619 U 44069 Standard profiles Testing conditions IP (PGI 2 ) cellul ar Ref. 2228 Agonist effect Ref. 2229 Antagonist effect Q 3 weeks Source human recombinant (CHO cells) Measured product cAMP Detection method HTRF Agonist effect Control iloprost (100 nM) Reference iloprost (EC 50 : 0.68 nM) Antagonist effect Stimulant iloprost (5 nM) Reference unavailable Boie, Y. et al. (1994) J. Biol. Chem., 269: 12173-12178. cAMP modulation (% of control) 100 50 0 -13 -12 -11 iloprost PGI2 PGE2 PGF2α -10 -9 -8 -7 -6 log [agonist] (M) [Solvent] must be kept ≤ 0.3% antagonist effect: no graph available Ordering information Assay list & index -11 -10 -9 -8 -7 -6 -5 -4 -12 -11 -10 -9 -8 -7
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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
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 and 60: 59 Cerep services ❚ opioid and op
Page 61 and 62: 61 NOP (ORL1) - agonist radioligand
Page 63: 63 platelet activating factor ❚ P
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
Page 111 and 112: 111 protein-tyrosine kinases [Rtk]
Page 113 and 114: 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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