in vitro PHARMACOLOGY 2011 CATALOG - Cerep

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44 in vitro pharmacology 2011 catalog ❚ Leukotrienes BLT 1 (LTB 4 ) - agonist radioligand binding Ref. 1209 Q 3 weeks Included in: Diversity profile BioPrint ® profile Organ safety profile Source Ligand Kd Non specific Reference human recombinant (CHO cells) [ 3 H]LTB 4 (0.2 nM) 0.2 nM LTB 4 (0.2 µM) LTB 4 (IC 50 : 0.2 nM) Yokomizo, T. et al. (2001) J. Biol. Chem., 276: 12454-12459. specific binding (% of control) 100 50 0 -11 -10 -9 -8 -7 -6 -5 log [drug] (M) LTB4 LTD4 U75302 BLT 1 (LTB 4 ) cellul ar Ref. 1245 Agonist effect Ref. 1837 Antagonist effect Q 3 weeks Source human recombinant (CHO cells) Measured product intracellular [Ca 2+ ] Detection method fluorimetry Agonist effect Control LTB 4 (100 nM) Reference LTB 4 (EC 50 : 1.2 nM) Antagonist effect Stimulant LTB 4 (10 nM) Reference unavailable Yokomizo, T. et al. (2000) J. Exp. Med., 192: 421-431. Ca 2+ mobilization (% of control) 100 50 0 -11 LTB 4 LTC4 LTD4 -10 -9 -8 -7 log [agonist] (M) [Solvent] must be kept ≤ 0.1% antagonist effect: no graph available CysLT 1 (LTD 4 ) - agonist radioligand binding Ref. 0086 Q 3 weeks Included in: Diversity profile BioPrint ® profile Organ safety profile Source Ligand Kd Non specific Reference human recombinant (CHO cells) [ 3 H]LTD 4 (0.3 nM) 0.24 nM LTD 4 (1 µM) LTD 4 (IC 50 : 0,335 nM) Martin V. et al. (2001) Biochem. Pharmacol., 62: 1193-1200. specific binding (% of control) -12 -11 -12 -11 -11 -10 100 -12 -11 -9 -8 -7 -6 -5 -4 -10 -9 -8 -7 -10 -9 -8 -7 50 -10 -9 -8 -7 -6 -5 -9 -8 -7 -6 -5 -10 -4 0 -11 -10 -9 -8 -7 -6 -5 -4 -12 -11 -10 -9 -8 -7 -6 -5 -4 -3 -12 -11 -10 -9 -8 -7 -6 log [drug] (M) LTD4 LTB4 MK 571 CysLT 1 (LTD 4 ) cellul ar Ref. 1383 Agonist effect Ref. 1607 Antagonist effect Q 3 weeks Source human recombinant (CHO cells) Measured product intracellular [Ca 2+ ] Detection method fluorimetry Agonist effect Control LTD 4 (10 nM) Reference LTD 4 (EC 50 : 0.33 nM) Antagonist effect Stimulant LTD 4 (1 nM) Reference MK 571 (IC 50 : 126 nM) Sarau, H.M. et al. (1999) Mol. Pharmacol., 56: 657-663. Ca 2+ mobilization (% of control) 100 50 0 100 50 0 -11 -10 -9 -8 -7 -6 -8 -7 -6 log [agonist] (M) log [antagonist] (M) LTD4 MK 571 LTC4 LTB 4 [Solvent] must be kept ≤ 0.1% CysLT 2 (LTC 4 ) - agonist radioligand Source human recombinant (HEK-293 cells) Ligand [ 3 H]LTD 4 (1 nM) Kd 1.5 nM Non specific LTD 4 (1 µM) binding Reference LTC 4 (IC 50 : 7.2 nM) Ref. 2050 Q 3 weeks Hui, Y. et al. (2001) J. Biol. Chem., 276: 47489-47495. specific binding (% of control) -11 -10 -9 -8 -7 -6 -5 -4 -13 -12 -11 -10 -9 -8 -7 -6 -5 50 -11 -10 -9 -8 -7 -6 -9 -8 -7 -6 -5 -10 -4 -12 -11 -10 -9 -8 -7 -6 -12 -11 100 -100 -9 -8 -7 -6 -5 -12 -11 -10 -9 -8 -7 -6 -5 -4 log [drug] (M) LTC4 LTD4 -12 -11 -10 -9 -8 -7 LTB -6 -5 -4 -3 4 MK 571 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 Assay developed in 2010 New assay conditions Human Q Standard turnaround time
45 leukotrienes ❚ CysLT 2 (LTC 4 ) cellul ar Ref. 2051 Agonist effect Ref. 2052 Antagonist effect Q 3 weeks Source human recombinant (HEK-293 cells) Measured product intracellular [Ca 2+ ] Detection method fluorimetry Agonist effect Control LTC 4 (300 nM) Reference LTC 4 (EC 50 : 18 nM) Antagonist effect Stimulant LTC 4 (100 nM) Reference unavailable Takasaki, J. et al. (2000) Biochem. Biophys. Res. Commun., 274: 316-322. Ca 2+ mobilization (% of control) 100 50 0 -11 -10 LTC4 LTD4 LTB4 -9 -8 -7 -6 log [agonist] (M) [Solvent] must be kept ≤ 0.1% antagonist effect: no graph available Cerep services Receptors [GPCRs] -11 -10 -9 -8 -7 -6 -5 -4 -12 -11 -10 -9 -8 -7 -11 -10 -9 -8 -7 -6 -5 -4 -12 -11 -10 -9 -8 -7 -6 -5 -4 -3 -12 -11 -12 -11 -10 -9 -8 -7 -10 -9 -8 -7 -6 -5 Ion channels -9 -8 -7 -6 -5 -10 -4 ❚ Lysophospholipid Transporters LPA 1 - agonist radioligand Source human recombinant (CHO cells) ❚ lysophosphatidic acid Ligand [ 3 H]LPA (2 nM) binding Kd 19 nM Ref. 1468 Non specific LPA (10 µM) Q 3 weeks Reference LPA (IC 50 : 42.5 nM) Included in: Organ safety profile An, S. et al. (1997) Biochem. Biophys. Res. Commun., 231: 619-622. specific binding (% of control) 100 50 0 LPA phosphatidic acid SEW 2871 S 1P -10 -9 -8 -7 -6 -5 -4 log [drug] (M) Kinases Epigenetic & DNA-related enzymes LPA 2 ❚ lysophosphatidic acid cellul ar Ref. 3171 Agonist effect Ref. 3172 Antagonist effect Q 3 weeks Source human recombinant (CHO cells) Measured product intracellular [Ca 2+ ] Detection method fluorimetry Agonist effect Control LPA (1 µM) Reference LPA (EC 50 : 3.5 nM) Antagonist effect Stimulant LPA (30 nM) Reference unavailable Heise, C.E. et al. (2001) Mol. Pharmacol., 60: 1173-1180. 1 [Solvent] must be kept 0.3% Other enzymes Specialized cellular assays LPA 3 ❚ lysophosphatidic acid cellul ar Ref. 3158 Agonist effect Ref. 3170 Antagonist effect Q 3 weeks Source human recombinant (CHO cells) Measured product intracellular [Ca 2+ ] Detection method fluorimetry Agonist effect Control LPA (1 µM) Reference LPA (EC 50 : 6.4 nM) Antagonist effect Stimulant LPA (30 nM) Reference VPC 32183 (IC 50 : 3.9 µM) Heise, C.E. et al. (2001) Mol. Pharmacol., 60: 1173-1180. 1 [Solvent] must be kept 0.3% Standard profiles Testing conditions S 1 P 1 ❚ sphingosine 1-phosphate cellul ar Ref. 3269 Agonist effect Ref. 3271 Antagonist effect Q 3 weeks Source human recombinant (CHO cells) Measured product impedance Detection method cellular dielectric spectroscopy Agonist effect Control S 1 P (300 nM) Reference S 1 P (EC 50 : 4 nM) Antagonist effect Stimulant S 1 P (10 nM) Reference VPC 23019 (IC 50 : 150 nM) Davis, M.D., et al. (2005) J. Biol. Chem., 11: 9833-9841. [Solvent] must be kept 0.1% 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: 43 H 3 - agonist radioligand Source
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 81 and 82: 81 LXRb - agonist radioligand bindi
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
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99 kainate - agonist radioligand bi
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101 ❚ purinergic channels Cerep s
Page 103 and 104:
103 Cerep services transporters Rec
Page 105 and 106:
105 norepinephrine ❚ norepinephri
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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
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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 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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