in vitro PHARMACOLOGY 2011 CATALOG - Cerep

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192 in vitro pharmacology 2011 catalog ❚ Cell migration PDGF-stimulated A7r5 migration 1. 5 cellul ar Ref. 0250 [CUSTOM OFFER] Source A7r5 cells Stimulant PDGF-BB (100 ng/mL) Measured product cells stained with crystal violet Detection method photometry Reference tyrphostin 9 (5 µM) Koyama, N. et al. (1994) Circ. Res., 75: 682-691. absorbance at 550 nm 1. 0 0. 5 0. 0 - + + + + PDGF 100 ng/mL - - 2x10 -7 2x10 -6 5x10 -6 Tyrphostin 9 (M) PDGF-stimulated AoSMC migration 2. 0 cellul ar Ref. 0344 [CUSTOM OFFER] Source AoSMC Stimulant PDGF-BB (100 ng/mL) Measured product cells stained with crystal violet Detection method photometry Reference tyrphostin 9 (5 µM) Koyama, N. et al. (1994) Circ. Res., 75: 682-691 absorbance at 550 nm 1. 5 1. 0 0. 5 0. 0 - + + + + + PDGF 100 ng/mL - - 2x10 -7 2x10 -6 5x10 -6 10 -5 Tyrphostin 9 (M) ❚ Cell proliferation serum-stimulated A7r5 proliferation cellul ar Ref. 0251 [CUSTOM OFFER] Source A7r5 cells Stimulant FCS (10 %) Measured product BrdU incorporation Detection method Reference EIA nitrendipine (IC 50 : 52 µM) Handler, J.A. et al. (1990) J. Biol. Chem., 265: 3669-3673. [ 3 H]BrdU incorporation (% of control) 100 50 0 -7 -6 -5 -4 log [drug] (M) nitrendipine PDGF-stimulated A7r5 proliferation cellul ar Ref. 0352 [CUSTOM OFFER] Source Stimulant Tracer Measured product A7r5 cells PDGF-BB (50 ng/mL) [ 3 H]TMD (0.25 µCi) [ 3 H]TMD incorporation Detection method scintillation counting Reference tyrphostin 9 Koyama, N. et al. (1994) Circ. Res., 75: 682-691. [ 3 H]TMD incorporation (dpm) 15000 10000 5000 0 - + tyrphostin 3x10 -7 nitrendipine 10 -5 verapamil 3x10 -5 EGF-stimulated A-431 proliferation cellul ar Ref. 0252 [CUSTOM OFFER] Source A-431 cells Stimulant EGF (1 ng/mL) Tracer [ 3 H]TMD (0.05 µCi) Measured product [ 3 H]TMD incorporation Detection method scintillation counting Reference staurosporine (IC 50 : 3 nM) [Solvent] must be kept ≤ 0.1% Handler, J.A. et al. (1990) J. Biol. Chem., 265: 3669-3673. [ 3 H]TMD incorporation (dpm) 100 50 0 -10 -9 -8 log [drug] (M) staurosporine
193 PDGF-stimulated Balb/c 3T3 proliferation cellul ar Ref. 0253 [CUSTOM OFFER] Source Stimulant Tracer Measured product Detection method Balb/c 3T3 cells PDGF-BB (3 ng/mL) [ 3 H]TMD (1 µCi) [ 3 H]TMD incorporation scintillation counting Reference cycloheximide (IC 50 : 100 nM) Handler, J.A. et al. (1990) J. Biol. Chem., 265: 3669-3673. [ 3 H]TMD incorporation (dpm) cell proliferation ❚ 100 50 0 cycloheximide -10 -9 -8 -7 -6 -5 -4 log [drug] (M) Cerep services Receptors VEGF-stimulated HUV-EC-C proliferation cellul ar Ref. 0937 [CUSTOM OFFER] Source HUV-EC-C cells Stimulant VEGF (10 nM) Tracer [ 3 H]TMD (0.2 µCi) Measured product [ 3 H]TMD incorporation Detection method scintillation counting Reference TNFα (IC 50 : 4.4 pM) [Solvent] must be kept ≤ 0.1% Mauerhoff, T. et al. (1994) Tumori, 80: 301-305. [ 3 H]TMD incorporation (dpm) 100 50 0 -50 -14 -13 -12 -11 -10 -9 -8 -7 -6 -5 -4 log [drug] (M) TNFα staurosporine Ion channels Transporters PHA-stimulated PBMC proliferation cellul ar Ref. 0254 [CUSTOM OFFER] Source PBMC Stimulant PHA (2 µg/mL) Tracer [ 3 H]TMD (1 µCi) Measured product [ 3 H]TMD incorporation Detection method scintillation counting Reference staurosporine (IC 50 : 19 nM) [Solvent] must be kept ≤ 0.1% Gougerot-Pocidalo, M.A. et al. (1988) Immunology, 64: 281-288. [ 3 H]TMD incorporation (% of control) 100 50 0 staurosporine -10 -9 -8 -7 -6 log [drug] (M) Kinases Epigenetic & DNA-related enzymes ❚ Cell viability Other enzymes cell viability Source U-937, HUVEC, PBMC, THP-1, A7r5, HL-60 or SK-N-SH cells Substrate MTT (0.5 mg/mL) Measured product formazan Detection method photometry cellul ar 0 Reference erythromycin or PMA erythromycin 0.1 0.3 1.0 Ref. 0274 n To be combined with secretion assays [erythromycin] (mg/mL)-24h incubation [CUSTOM OFFER] Mosmann, T. (1983) J. Immunol. Met., 65: 55-63. ❚ Cellular models such as human primary hepatocytes, and other technology such alamarBlue are available: see ADME-Tox & PK 2011 catalog PBMC viability (% of viable cells) 100 50 Specialized cellular assays Standard profiles 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 ❚ Europe: +33 (0)5 49 89 30 00 – USA: +1 (425) 895 8666 – Japan: +81 (0)3 3354 4026 – China: +86 21 5132 0568 Human Q Standard turnaround time [CUSTOM OFFER] Please contact us at: customresearch@cerep.com 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
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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
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 and 174: 173 proteases [metalloproteases]
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: 191 expression of endothelial adhes
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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