in vitro PHARMACOLOGY 2011 CATALOG - Cerep

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216 in vitro pharmacology 2011 catalog lipid peroxydation 190 ❚ assay list & index galanin (non-selective)- agonist radioligand 38 GCK (MAP4K2) 145 GHRH 41 GLP-1 39 GLP-1 - agonist radioligand 39 GLP-2 39 glucagon 40 Glucagon 39 glucagon - agonist radioligand 40 Glutamate 86,98 Glycine 87,99 glycine (strychnine-insensitive)- antagonist radioligand 87,99 Glycoprotein hormone 40 GnRH (LH-RH)- agonist radioligand 40 Gonadotrophin-releasing hormone 40 GPCRs 13 GPCRs (tool-box) 6 GPR119 62 G protein-coupled receptors 13 GR - agonist radioligand 80 GRK2 (ADRBK1) 138 GRK3/BARK2 (ADRBK2) 138 GRK5 138 Growth factors 87 Growth hormone-releasing hormone 41 GSK3a 127 GSK3b 127,128 guanylyl cyclase (activator effect) 181 guanylyl cyclase (inhibitor effect) 181 [H] H 1 41 H 1 - antagonist radioligand 41 H 2 42 H 2 - antagonist radioligand 42 H 2 - inverse agonist effect 42 H 2 O 2 scavenging 190 H 2 O 2 secretion 190 H 3 43 H 3 - agonist radioligand 42,43 H 4 43 H 4 - agonist radioligand 43 HCK 120 HDAC1 158 HDAC2 158 HDAC3 159 HDAC4 159 HDAC5 159 HDAC6 159 HDAC7 159 HDAC8 159 HDAC9 160 HDAC10 160 HDAC11 160 HDACs 158 HER2/ErbB2 kinase 113 HER4/ErbB4 kinase 113 hERG (automated patch-clamp) 94 hERG (conventional patch-clamp) 94 hERG (membrane preparation) - antagonist radioligand 94 HGK (MAP4K4) 145 high throughput screening 4 HIPK2 128 HIPK3 128 HIPK4 128 Histamine 41 histamine release (activator effect) 185 histamine release (inhibitor effect) 185 HIV-1 protease 171 HMG-CoA reductase 183 HNE (human neutrophil elastase) 168 HNMT (histamine N-methyl transferase) 179 HTRF ® 107 [I] I 1 - agonist radioligand 88 I 2 - antagonist radioligand 88 IC 50 /EC 50 follow-up studies 204,205,209 IFN-g secretion (inhibitor effect) 188 IGF1Rb kinase 114 IGF1R kinase 114 IKKa 152 IKKb 152 IKKe (IKBKE) 152 IL-1b - agonist radioligand 84 IL-1β secretion (inhibitor effect) 188 IL-2 - agonist radioligand 84 IL-2 secretion (inhibitor effect) 189 IL-4 - agonist radioligand 84 IL-4 secretion (inhibitor effect) 189 IL-5 secretion (inhibitor effect) 189 IL-6 - agonist radioligand 84 IL-6 secretion (inhibitor effect) 189 IL-8 secretion (inhibitor effect) 188 IL-10 secretion (inhibitor effect) 189 Imidazoline 88 inducible NOS 176,177 Inositol phosphate 181 Insulin 88 insulin - agonist radioligand 88 Intracellular ligand-gated channels 102 in vitro ADME profiling 4 in vitro pharmacology assays 11 in vitro safety profiling 4 in vivo PK 4 ion channel patch-clamp assays 95 Ion channels 93 Ion transport systems 186 IP 3 - agonist radioligand 102,181 IP (PGI 2 ) 65 IP (PGI 2 )- agonist radioligand 65 IRAK1 149 IRAK4 150 IRK (InsR) 114 IRK (InsRb) 114 IRR kinase 114 ITK 120 [J] JAK1 121 JAK2 121 JAK3 121 JNK1 128 JNK1/3 129 JNK2 128 JNK3 129 [K] K + channels 94 kainate - agonist radioligand 86,99 kallikrein 168 kappa (KOP) 60 kappa (KOP)- agonist radioligand 59 K ATP 95 K ATP - antagonist radioligand 94 KDR kinase (VEGFR2) 115 Kinases 107 K V - antagonist radioligand 95 [L] LANCEUltra ® 107 Lck kinase 121 lead optimization (or SAR) profiling 4 Leukotrienes 44 LIMK1 150 Locations (Cerep sites) back cover LPA 1 - agonist radioligand 45 LPA 2 45 LPA 3 45 LRRK2 150 LTB 4 secretion (inhibitor effect) 187 LTC 4 secretion (inhibitor effect) 187 LTK 115 LXRb - agonist radioligand 81 Lyn A kinase 121 Lyn B kinase 121 Lysophosphatidic acid 45 Lysophospholipid 45 [M] M 1 50 M 1 - antagonist radioligand 50 M 2 51 M 2 - agonist radioligand 51 M 2 - antagonist radioligand 51 M 2 - inverse agonist effect 51 M 3 52 M 3 - antagonist radioligand 51 M 4 52 M 4 - agonist radioligand 52 M 4 - antagonist radioligand 52 M 4 - inverse agonist effect 52 M 5 53 M 5 - agonist radioligand 53 M 5 - antagonist radioligand 53 MAO-A 179 MAO-A - antagonist radioligand 180 MAO-B 180 MAO-B - antagonist radioligand 180 MAPKAPK2 133 MAPKAPK5 (PRAK) 133 MARK1 133 MARK2 133 MARK3 133 MARK4 133 master service agreement 208 MC 1 47 MC 1 - agonist radioligand 47 MC 2 47 MC 3 48 MC 3 - agonist radioligand 47 MC 4 48 MC 4 - agonist radioligand 48 MC 4 - inverse agonist effect 48 MC 5 48 MCH 1 46 MCH 1 - agonist radioligand 46 MCH 2 47 MCH 2 - agonist radioligand 46 MEK1 145 MEK1 (MAP2K1) 145 MEK5 (MAP2K5) 145 MEKK3 (MAP3K3) 146 MEKK4 (MAP3K4) 146 Melanin concentrating hormone 46 Melanocortin 47 Melatonin 49,89 MELK 134 Membrane ligand-gated channels 97 Mer kinase 115 Metalloproteases 171 MINK 146 Miscellaneous enzymes 182 MKK4/JNK1 146 MKK4/JNK2 146 MKK6 146 MKK6/p38a (mutant active) 147 MLK1 150 MLK2 (MAP3K10) 150 MMP-1 172 MMP-2 172
217 MMP-3 172 MMP-7 172 MMP-8 172 MMP-9 173 MMP-12 173 MMP-13 173 MNK1 134 MNK2 134 M (non-selective)- antagonist radioligand 50 molecular weight (MW) 208,209,210 Monoamine & neurotransmitter synthesis & metabolism 179 Monomamine & neurotransmitter release 185 MOS kinase 152 Motilin 49 motilin - agonist radioligand 49 motilin 50 MRCKa 138 MSK1 139 MSK2 139 MST1 kinase (STK4) 147 MST2 kinase 147 MST3 kinase 147 MST4 kinase 147 MT 1 (ML 1A ) 49 MT 1 (ML 1A )- agonist radioligand 49 MT1-MMP (MMP-14) 173 MT 2 (ML 1B ) 49 MT 2 (ML 1B )- agonist radioligand 49 MT 3 (ML 2 )- agonist radioligand 89 mTOR kinase (FRAP1) 156 mu (MOP) 60 mu (MOP)- agonist radioligand 60 mu (MOP)- antagonist radioligand 60 Muscarinic 50 MusK 115 myeloperoxidase 183 MYT1 kinase 153 [N] Na + 96 Na + /Ca 2+ antiport 186 Na + channels 96 Na + /H + antiport 187 Na + /K + - ATPase pump 186 Na + /K + /Cl – cotransport 187 Na + - site 2 - antagonist radioligand 96 Na V 1.5 (automated patch-clamp) 96 Na V 1.5 (conventional patch-clamp) 96 NDR1 kinase 139 NEK1 153 NEK2 153 NEK4 153 NEK6 153 NEK7 153 Neurokinin 53 Neuromedin U 55 Neuropeptide S 56 Neuropeptide W/neuropeptide B 56 Neuropeptide Y 56 Neurotensin 58 neutral endopeptidase 173 N-formyl peptide 36 Nicotinic 89,100 NIK 147 NIM1 kinase (MGC42105) 134 NK 1 53,54 NK 1 - agonist radioligand 53 NK 2 54 NK 2 - agonist radioligand 54 NK 3 55 NK 3 - agonist radioligand 55 NK 3 - antagonist radioligand 54 NMDA - antagonist radioligand 86,99 NMU1 55 NMU2 - agonist radioligand 56 N muscle-type - antagonist radioligand 90,100 N neuronal (a4b2)- agonist radioligand 89,100 N neuronal (a7) - antagonist radioligand 89,90,100 non-recombinant models (tool-box) 5 Non-steroid nuclear receptors 80 NOP (ORL1) 61 NOP (ORL1)- agonist radioligand 61 Norepinephrine 104 norepinephrine release (activator effect) 185 norepinephrine transporter - antagonist radioligand 104 norepinephrine uptake 105 NO synthases 176 NPBW1 56 NPS 56 NT (non-selective) 58 NT (non-selective)- agonist radioligand 58 NTS 1 (NT 1 ) 58 NTS 1 (NT 1 )- agonist radioligand 58 NTS 2 58 NuaK1 (ARK5) 134 nuclear receptors 79 [O] Opioid and opioid-like 59 opioid (non-selective)- antagonist radioligand 59 Ordering information 208 Orexin 61 Orphans (Class A) 62 OT 77 Other enzymes 163 Other kinases 151 Other receptors 83 OX 1 61 OX 1 - agonist radioligand 61 OX 2 62 OX 2 - agonist radioligand 62 [P] P2X 90,101 P2X - agonist radioligand 90,101 P2Y - agonist radioligand 67 P2Y 1 67 P2Y 2 67 P2Y 4 67 P2Y 6 68 P2 Y - agonist radioligand 67 p38a kinase 129 p38b2 kinase (SAPK2b2) 129 p38g kinase 129 p38d kinase 130 p38 MAPK 129 p70S6K 139 p70S6Kb 139 PAC 1 (PACAP) 76 PAC 1 (PACAP)- agonist radioligand 75 PAF 63 PAF - agonist radioligand 62 PAK1 148 PAK2 148 PAK4 148 PAR1 66 PAR1 - agonist radioligand 66 PAR2 67 PAR2 - agonist radioligand 66 Parathyroid hormone 62 PASK 134 PCP - antagonist radioligand 86,99 PCTAIRE1 kinase 130 PDE1B 174 PDE2A 174 PDE3A 174 PDE3B 174 PDE4A 1A 175 PDE4B 1 175 assay list & index ❚ PDE4D 2 175 PDE5 (non-selective) 175 PDE6 (non-selective) 175 PDE7A 175 PDE8A 176 PDE10A 1 176 PDE11A 4 176 PDGF - agonist radioligand 87 PDGFR kinase 115 PDGFRa kinase 115 PDGFRb kinase 116 PDGF-stimulated A7r5 migration 192 PDGF-stimulated A7r5 proliferation 192 PDGF-stimulated AoSMC migration 192 PDGF-stimulated Balb/c 3T3 proliferation 193 PDK1 139 PEK (EIF2AK3) 154 PGE 2 secretion (inhibitor effect) 187 PGI 2 secretion 188 PHA-stimulated PBMC proliferation 193 PhKg1 135 PhKg2 135 phosphatase 1B (PTP1B) 163 phosphatase 2A (PP2A) 163 phosphatase 2B 164 phosphatase CD45 164 phosphatase CDC25A 164 phosphatase CDC25B 164 phosphatase CDC25C 164 phosphatase DEP1 (PTPRJ) 164 phosphatase LAR (PTPRF) 165 phosphatase MEG1 (PTPN4) 165 phosphatase MEG2 (PTPN9) 165 phosphatase MKP1 165 phosphatase MKP2 165 phosphatase MKP3 165 phosphatase MKP6 166 phosphatase PEST (PTPN12) 166 phosphatase PP1a 163 phosphatase PTPb (PTPRB) 166 phosphatase PTPg (PTPRG) 166 phosphatase PTPµ (PTPRM) 166 Phosphatases 163 phosphatase SHP1 (PTPN6) 166 phosphatase SHP2 (PTPN11) 167 phosphatase TC-PTP (PTPN2) 167 phosphatase VHR (DUSP3) 167 Phosphodiesterases 174 Phospholipase C 182 Pim1 kinase 135 Pim2 kinase 135 (in vivo) PK 4 PK 1 63 PK 2 63 PKA 140 PKCa 140 PKCb1 140 PKCb2 140 PKCg 140 PKCd 140 PKCe 141 PKCz 141 PKCh 141 PKCq 141 PKCi 141 PKD1 (PKCµ) 135 PKD2 135 PKD3 136 PKG1a 141 PKG1b 142 PKG2 142 PKN1 142 PKN2 142 PKR (EIF2AK2) 154 PLA 2 (See sPLA 2) Platelet activating factor 62 PLC 182 PLK1 154 PLK2 154 Cerep services Receptors Ion channels Transporters Kinases Epigenetic & DNA-related enzymes Other enzymes Specialized cellular assays Standard profiles Testing conditions Ordering information Assay list & index
Page 1 and 2:
in vitro pharmacology 2011 catalog
Page 3 and 4:
Cerep services p. 4 Receptors [GPC
Page 5 and 6:
5 ❚ tool-box for cell-based assay
Page 7 and 8:
7 ❚ profile design Cerep offers a
Page 9 and 10:
9 ❚ data online A powerful web-ba
Page 11 and 12:
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 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 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 79 and 80:
Page 81 and 82:
81 LXRb - agonist radioligand bindi
Page 83 and 84:
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
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 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 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: 215 CDK5/p35 124 CDK6 (cycD3) 125 C
Page 219 and 220: contacts ❚ france [Laboratories]
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