in vitro PHARMACOLOGY 2011 CATALOG - Cerep

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172 in vitro pharmacology 2011 catalog ❚ proteases [metalloproteases] ECE-1 ❚ metalloprotease tissue Ref. 0313 Q 4 weeks Source rabbit saphenous artery Agonist big endothelin-1 (pD 2 = 8.5) Antagonist phosphoramidon (pA 2 = 8) Test concentrations [Solvent] must be kept ≤ 0.1% 3 concentrations, n=2 (2 tissues) for both activities Auguet, M. et al. (1992) Eur. J. Pharmacol., 224: 101-102. tension (% of max.) 100 50 0 -9 -8 -7 log [agonist] (M) phosphoramidon none 0.01 µM 0.1 µM 1 µM MMP-1 ❚ metalloprotease Ref. 0510 Q 3 weeks Included in: Non-kinase enzyme profile BioPrint ® profile Organ safety profile Source human recombinant (E. coli) Substrate DNP-P-Cha-GC(Me)-HAK(n-Me-Abz)-NH 2 (10 µM) Measured product Cys(Me)-HAK(n-Me-Abz)-NH 2 Detection method Reference fluorimetry GM6001 (IC 50 : 1.9 nM) Bickett, D.A. et al. (1993) Anal. Biochem., 212: 58-64. enzyme activity (% of control) 100 50 0 -12 -11 -10 -9 -8 -7 log [drug] (M) GM 6001 TIMP-1 TIMP-2 MMP-2 ❚ metalloprotease Ref. 0489 Q 3 weeks Included in: BioPrint ® profile Source human recombinant Substrate NFF-2 (10 µM) Measured product Mca-RPKPYA Detection method fluorimetry Reference GM6001 (IC 50 : 1.6 nM) Nagase, N. et al. (1994) J. Biol. Chem., 269: 20952-20957. enzyme activity (% of control) 100 50 0 -11 -10 -9 -8 -7 log [drug] (M) GM 6001 TIMP-2 TIMP-1 MMP-3 ❚ metalloprotease Ref. 0490 Q 3 weeks Included in: Non-kinase enzyme profile Source human recombinant Substrate NFF-2 (10 µM) Measured product Mca-RPKPYA Detection method fluorimetry Reference GM6001 (IC 50 : 35 nM) Nagase, N. et al. (1994) J. Biol. Chem., 269: 20952-20957. enzyme activity (% of control) 100 50 GM 6001 0 TIMP-1 TIMP-2 -12 -11 -10 -9 -8 -7 -6 log [drug] (M) MMP-7 ❚ metalloprotease Ref. 0502 Q 3 weeks Source human recombinant (E. coli) Substrate MMP-2/MMP-7 substrate (5 µM) Measured product Mca-PLG Detection method fluorimetry Reference GM6001 (IC 50 : 11 nM) Quesada, A.R. et al. (1997) Clin. Exp. Metastasis, 15: 26-32. MMP-8 ❚ metalloprotease Ref. 0643 Q 6 weeks Source human neutrophils Substrate Mca-P-Cha-G-Nva-HA-Dpa-NH 2 (1 µM) Measured product Mca-P-Cha-G Detection method fluorimetry Reference GM6001 (IC 50 : 0.3 nM) Knauper, V. et al. (1996) J. Biol. Chem., 271: 1544-1550.
173 proteases [metalloproteases] ❚ MMP-9 ❚ metalloprotease Ref. 0491 Q 3 weeks Included in: Non-kinase enzyme profile BioPrint ® profile Source human recombinant Substrate NFF-2 (10 µM) Measured product Mca-RPKPYA Detection method fluorimetry Reference GM6001 (IC 50 : 1.1 nM) Nagase, N. et al. (1994) J. Biol. Chem., 269: 20952-20957. enzyme activity (% of control) 100 50 0 -12 -11 -10 -9 -8 -7 log [drug] (M) GM 6001 TIMP-1 TIMP-2 Cerep services Receptors MMP-12 ❚ metalloprotease Ref. 0511 Q 6 weeks Source Substrate Measured product Detection method Reference human recombinant MMP fluorescent substrate (10 µM) Dnp-AG fluorimetry GM6001 (IC 50 : 0.75 nM) Hiller, O. et al. (2000) J. Biol. Chem., 275: 33008-33013. enzyme activity (% of control) 100 -10 -9 -8 -7 -6 -5 -4 50 -11 -10 -9 -8 -7 -6 GM 6001 NNGH 0 TIMP-1 -12 -11 -10 -9 -8 -7 -6 log [drug] (M) Ion channels Transporters MMP-13 ❚ metalloprotease Ref. 0632 Q 6 weeks Source Substrate Measured product Detection method Reference human recombinant (Spodoptera frugiperda) MMP-13 substrate (2 µM) Mca-P-Cha-G fluorimetry GM6001 (IC 50 : 0.31 nM) Knauper, V. et al. (1996) J. Biol. Chem., 271: 1544-1550. -10 -9 -8 -7 -6 -5 -4 -11 -10 -9 -8 -7 -6 -12 -11 -10 -6 -9 -8 -7 Kinases Epigenetic & DNA-related enzymes MT1-MMP (MMP-14) ❚ metalloprotease Ref. 0670 Q 3 weeks Source human recombinant Substrate MMP-14 substrate (2 µM) Measured product Mca-PLA Detection method fluorimetry Reference GM6001 (IC 50 : 3.1 nM) Mucha, A. et al. (1998) J. Biol. Chem., 273: 2763-2768. Other enzymes Specialized cellular assays neutral endopeptidase ❚ metalloprotease Ref. 0509 Q 3 weeks Included in: Non-kinase enzyme profile BioPrint ® profile Organ safety profile Source Substrate Measured product Detection method Reference HUV-EC-C cells DAGNPG (50 µM) Dansyl-D-AG fluorimetry thiorphan (IC 50 : 0.94 nM) Graf, K. et al. (1998) Basic Res. Cardiol., 93: 11-17. Standard profiles Testing conditions TACE ❚ metalloprotease Ref. 0702 Q 3 weeks Included in: Non-kinase enzyme profile Organ safety profile Source human recombinant (insect cells) Substrate TACE substrate II (4 µM) Measured product Mca-PLAQA Detection method fluorimetry Reference GM6001 (IC 50 : 40 nM) Van Dyk, D.E. et al. (1997) Bioorg. Med. Chem. Lett., 7: 1219-1224. enzyme activity (% of control) 100 50 0 -11 -10 -9 -8 -7 -6 log [drug] (M) GM 6001 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]
Page 121 and 122: 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: 171 proteases [aspartic proteases]
Page 175 and 176: phosphodiesterases ❚ 175 PDE4A 1
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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