in vitro PHARMACOLOGY 2011 CATALOG - Cerep

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74 in vitro pharmacology 2011 catalog ❚ somatostatin sst 2 - agonist radioligand binding Ref. 2339 Q 6 weeks Source Ligand Kd Non specific Reference IMR32 cells (endogenous) [ 125 I]Tyr 11 -somatostatin-14 (0.04 nM) 0.2 nM seglitide (1 µM) seglitide (IC 50 : 0.2 nM) O’Dorisio, M.S. et al. (1994) Cell Growth Differ., 5: 1-8. specific binding (% of control) 100 50 0 -12 -11 -10 -9 -8 -7 -6 -5 log [drug] (M) seglitide somatostatin-14 CYN 154806 BIM 23027 sst 4 - agonist radioligand binding Ref. 0482 Q 3 weeks Included in: BioPrint ® profile Organ safety profile Source Ligand Kd Non specific Reference human recombinant (CHO cells) [ 125 I]Tyr 11 -somatostatin-14 (0.1 nM) 5.9 nM somatostatin-14 (1 µM) somatostatin-14 (IC 50 : 1.4 nM) Rohrer, L. et al. (1993) Proc. Natl. Acad. Sci. USA, 90: 4196-4200. specific binding (% of control) 100 50 0 -11 -10 -9 -8 -7 -6 -5 log [drug] (M) ▲ somatostatin-14 ● [D-Trp 8 ]- somatostatin ■ somatostatin-28 ▼ BIM 23056 sst 4 cellul ar Ref. 2095 Ref. 2103 Q 3 weeks Agonist effect Antagonist effect Source human recombinant (CHO cells) Measured product cAMP Detection method HTRF Agonist effect Control somatostatin-14 (100 nM) Reference somatostatin-14 (EC 50 : 0.21 nM) Antagonist effect Stimulant somatostatin-14 (3 nM) Reference unavailable Engström, M. et al. (2005) J. Pharm. Exp. Ther., 312: 332-338. [Solvent] must be kept 0.3% sst 5 - agonist radioligand Source human recombinant (CHO cells) Ligand [ 125 I]Tyr 11 -somatostatin-14 (0.1 nM) binding Kd 0.2 nM Ref. 0626 Non specific somatostatin-14 (1 µM) Q 3 weeks Reference somatostatin-14 (IC 50 : 0.76 nM) Included in: Organ safety profile Yamada, Y. et al. (1993) Biochem. Biophys. Res. Commun., 195: 844-852. specific binding (% of control) 100 50 0 log [drug] (M) -13 - 12 -11 - 10 -9 -8 -7 -6 somatostatin-14 [D-Trp 8 ]- somatostatin somatostatin-28 BIM 23056 sst 5 cellul ar Ref. 2087 Ref. 2088 Q 3 weeks Agonist effect Antagonist effect Source human recombinant (CHO cells) Measured product cAMP Detection method HTRF Agonist effect Control somatostatin-14 (300 nM) Reference somatostatin-14 (EC 50 : 6.1 nM) Antagonist effect Stimulant somatostatin-14 (100 nM) Reference unavailable Carruthers, A.M. et al. (1999) Brit. J. Pharmacol., 126: 1221-1229. [Solvent] must be kept 0.3% For some binding assays two models are available using either agonist or antagonist as radioligand. ❚ For radioligand binding assays, how should I choose between the agonist and the antagonist models when both are available? G-protein-coupled receptors have both high-affinity and low-affinity states that are bound differently by agonists and antagonists. Whereas the antagonists bind with an equal affinity to both affinity states, agonists bind poorly to the low affinity state of the receptor. Therefore, it is advisable to use an antagonist radioligand to evaluate the binding of antagonists knowing that this may fail to reveal the binding of agonists. On the other hand, an assay using an agonist radioligand is suitable to evaluate both agonists and antagonists. The testing of a compound in both assays and the comparison of its competition curves against each radioligand may provide information about its functional activity at the receptor.
75 ❚ thyrotropin releasing hormone TRH 1 - agonist radioligand binding Ref. 1616 Q 3 weeks Included in: Diversity profile Organ safety profile TRH 1 cellul ar Ref. 1617 Ref. 2057 Q 3 weeks Agonist effect Antagonist effect Source Ligand Kd Non specific Reference human recombinant (CHO cells) [ 3 H]Me-TRH (2 nM) 3.9 nM TRH (10 µM) TRH (IC 50 : 39 nM) Hinuma, S. et al. (1994) Biochem. Biophys. Acta., 1219: 251-259. Source human recombinant (CHO cells) Measured product intracellular [Ca 2+ ] Detection method fluorimetry Agonist effect Control TRH (100 nM) Reference TRH (EC 50 : 0.16 nM) Antagonist effect Stimulant TRH (1 nM) Reference unavailable Yamada, M. et al. (1993) Biochem. Biophys. Res. Com., 195: 737-745. specific binding (% of control) Ca 2+ mobilization (% of control) 100 50 0 100 50 0 -11 -10 -9 -8 -7 -6 -5 -12 -11 log [drug] (M) log [agonist] (M) TRH Me-TRH -10 -9 -8 -7 [Solvent] must be kept ≤ 0.1% TRH Me-TRH antagonist effect: no graph available Cerep services Receptors [GPCRs] Ion channels Transporters ❚ urotensin-ii UT - agonist radioligand binding Ref. 1386 Q 3 weeks Included in: BioPrint ® profile Organ safety profile Source Ligand Kd Non specific Reference human recombinant (CHO cells) [ 125 I]urotensin-II (0.1 nM) 0.29 nM urotensin-II (3 µM) urotensin-II (IC 50 : 0.98 nM) Maguire, J.J. et al. (2000) Brit. J. Pharmacol. 131: 441-446. -12 -11 -12 -11 specific binding (% of control) -11 -10 100 -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 50 0 -11 -10 log [drug] (M) -9 -8 -7 -6 -5 -4 -12 -11 -10 -9 -8 -7 -6 urotensin-II Kinases Epigenetic & DNA-related enzymes Other enzymes UT cellul ar Ref. 1376 Ref. 1836 Q 3 weeks Agonist effect Antagonist effect Source human recombinant (CHO cells) Measured product intracellular [Ca 2+ ] Detection method fluorimetry Agonist effect Control human urotensin-II (100 nM) Reference human urotensin-II (EC 50 : 2 nM) Antagonist effect Stimulant human urotensin-II (10 nM) Reference unavailable Herold, C.L. et al. (2003) Brit. J. Pharmacol., 139: 203-207. Ca 2+ mobilization (% of control) 100 50 0 -12 -11 -10 -9 -8 -7 log [agonist] (M) human urotensin-II [Orn 8 ]-urotensin-II rat urotensin-II [Solvent] must be kept ≤ 0.1% antagonist effect: no graph available Specialized cellular assays Standard profiles ❚ vasoactive intestinal peptide PAC 1 (PACAP) - agonist radioligand binding Ref. 1518 Q 3 weeks Included in: High-throughput profile Organ safety profile Source Ligand Kd Non specific Reference human recombinant (CHO cells) [ 125 I]PACAP 1-27 (0.015 nM) 0.092 nM PACAP 1-27 (100 nM) PACAP 1-38 (IC 50 : 0.13 nM) Ohtaki, T. et al. (1998) J. Biol. Chem., 273: 15464-15473. -12 -11 -12 -11 specific binding (% of control) -11 -10 100 -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 50 0 -11 -10 log [drug] (M) -9 -8 -7 -6 -5 -4 -12 -11 -10 -9 -8 -7 -6 -5 PACAP1-38 PACAP1-27 VIP Testing conditions 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
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 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: 73 5-HT 7 - agonist radioligand bin
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
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
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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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