in vitro PHARMACOLOGY 2011 CATALOG - Cerep

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174 in vitro pharmacology 2011 catalog ❚ Phosphodiesterases Cyclic nucleotide phosphodiesterases (PDEs), ubiquitously distributed in mammalian tissues, play a major role in cell signaling by hydrolyzing cAMP and/or cGMP. Due to their diversity and specific distribution at cellular and subcellular levels, PDEs can selectively regulate various cellular functions. Increased understanding of their function at the cell and molecular level provides an impetus for the development of isoenzyme selective inhibitors for the treatment of various diseases. Examples are PDE3 inhibitors for congestive heart failure, PDE4 inhibitors for inflammatory airways disease and the most well known, inhibitor for erectile dysfunction (Viagra). As PDEs are expressed in a variety of tissues, selectivity is a prerequisite for a therapeutically applicable PDE inhibitor. As an example, high selectivity for PDE5 inhibitors is important for treatment of erectile dysfunction to minimize the possibility of side effects that arise as a result of inhibition of other PDEs. Possible side effects include heart rate increase and vasodilation that are attributed to inhibition of PDE1 and PDE3, or blue-green vision disturbances that are attributed to inhibition of PDE6. In this context, Cerep has designed a high throughput profiling platform to determine the inhibitory activity and selectivity of compounds on the PDE superfamily The robustness, reproducibility and relevance of this platform was determined by screening a broad panel of commercially available reference inhibitors and known clinical drugs in three independent experiments. Poster available upon request. ❚ For cellular phosphodiesterase assays, please contact us at customresarch@cerep.com PDE1B Ref. 2431 Q 3 weeks Included in: Diversity profile Organ safety profile PDE high-throughput profile Source human recombinant (Sf9 cells) Substrate cGMP (240 nM) Measured product residual cGMP Detection method HTRF Reference calmidazolium (IC 50 : 2.2 µM) Bender, A.T. and Beavo, J.A. (2006) Pharmacol. Rev., 58: 488-520. PDE2A Ref. 2426 Q 3 weeks Included in: Non-kinase enzyme profile Diversity profile BioPrint ® profile Organ safety profile PDE high-throughput profile Source human recombinant (Sf9 cells) Substrate cAMP (40 nM) Measured product residual cAMP Detection method HTRF Reference EHNA (IC 50 : 1.56 µM) Bender, A.T. and Beavo, J.A. (2006) Pharmacol. Rev., 58: 488-520. PDE3A Ref. 2432 Q 3 weeks Included in: Non-kinase enzyme profile Diversity profile Organ safety profile PDE high-throughput profile Source human recombinant (Sf9 cells) Substrate cAMP (40 nM) Measured product residual cAMP Detection method HTRF Reference milrinone (IC 50 : 270 nM) Bender, A.T. and Beavo, J.A. (2006) Pharmacol. Rev., 58: 488-520. enzyme activity (% of control) 100 50 0 -12 -11 -10 -9 -8 -7 -6 -5 -4 log [drug] (M) milrinone cilostamide trequinsin rolipram PDE3B Ref. 2705 Q 3 weeks Included in: BioPrint ® profile PDE high-throughput profile Source human recombinant (Sf9 cells) Substrate cAMP (40 nM) Measured product residual cAMP Detection method HTRF Reference milrinone (IC 50 : 510 nM) Bender, A.T. and Beavo, J.A. (2006) Pharmacol. Rev., 58: 488-520. -10 -9 -8 -7 -6 -5 -4 -3 -12 -11 -10 -9 -8 -7 -6 -5 -4 -10 -9 -8 -7 -6 -10 -7 -9 -8 -6 -5 -4 -12 -11 -10 -6 -5 -9 -8 -7
phosphodiesterases ❚ 175 PDE4A 1A Ref. 2342 Q 3 weeks Included in: Organ safety profile PDE high-throughput profile Source human recombinant (Sf9 cells) Substrate cAMP (40 nM) Measured product residual cAMP Detection method HTRF Reference rolipram (IC 50 : 77 nM) Saldou, N. et al. (1998) Cell signal., 10: 427-440. Cerep services Receptors PDE4B 1 Ref. 2413 Q 3 weeks Included in: Organ safety profile PDE high-throughput profile Source human recombinant (Sf9 cells) Substrate cAMP (40 nM) Measured product residual cAMP Detection method HTRF Reference rolipram (IC 50 : 46 nM) Saldou, N. et al. (1998) Cell signal., 10: 427-440. Ion channels Transporters PDE4D 2 Ref. 2434 Q 3 weeks Included in: Non-kinase enzyme profile Diversity profile BioPrint ® profile Organ safety profile PDE high-throughput profile Source human recombinant (Sf9 cells) Substrate cAMP (40 nM) Measured product residual cAMP Detection method HTRF Reference rolipram (IC 50 : 48 nM) Saldou, N. et al. (1998) Cell signal., 10: 427-440. Kinases Epigenetic & DNA-related enzymes PDE5 (non-selective) Ref. 0204 Q 3 weeks Included in: Non-kinase enzyme profile Diversity profile BioPrint ® profile Organ safety profile PDE high-throughput profile Source human platelets Substrate [ 3 H]cGMP + cGMP (1 µM) Measured product [ 3 H]5'GMP Detection method scintillation counting Reference dipyridamole (IC 50 : 700 nM) Weishaar, R.E. et al. (1986) Biochem. Pharmacol., 35: 787-800. Other enzymes Specialized cellular assays PDE6 (non-selective) Ref. 0478 Q 3 weeks Included in: Non-kinase enzyme profile BioPrint ® profile PDE high-throughput profile Source bovine retina Substrate [ 3 H]cGMP + cGMP (2 µM) Measured product [ 3 H]5’GMP Detection method scintillation counting Reference zaprinast (IC 50 : 212 nM) Ballard, A. S. et al. (1998) J. Urol., 159: 2164-2171. enzyme activity (% of control) 100 50 zaprinast dipyridamole IBMX 0 milrinone -8 -7 -6 -5 -4 -9 log [drug] (M) Standard profiles Testing conditions PDE7A Ref. 2351 Q 3 weeks Included in: Organ safety profile PDE high-throughput profile Source human recombinant (Sf9 cells) Substrate cAMP (40 nM) Measured product residual cAMP Detection method HTRF Reference BRL 50481 (IC 50 : 617 nM) Smith, S.J. et al. (2004) Mol. Pharm., 66: 1679-1689 -10 -9 -8 -7 -6 -5 -4 -11 -10 -9 -8 -7 -6 -12 -11 -10 -6 -9 -8 -7 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
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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
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 and 162: 161 HDACs ❚ sirtuin 3 Source Subs
Page 163 and 164: 163 Cerep services Other enzymes Re
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: 173 proteases [metalloproteases]
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
Page 213 and 214: 213 assay list & index
Page 215 and 216: 215 CDK5/p35 124 CDK6 (cycD3) 125 C
Page 217 and 218: 217 MMP-3 172 MMP-7 172 MMP-8 172 M
Page 219 and 220: contacts ❚ france [Laboratories]
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in vitro PHARMACOLOGY 2011 CATALOG - Cerep

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