in vitro PHARMACOLOGY 2011 CATALOG - Cerep

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26 in vitro pharmacology 2011 catalog ❚ calcitonin gene-related peptide CGRP - agonist radioligand binding Ref. 0373 Q 3 weeks Included in: High-throughput profile Organ safety profile Source Ligand Kd Non specific Reference human recombinant (CHO cells) [ 125 I]hCGRPa (0.03 nM) 0.06 nM hCGRPa (1 µM) hCGRPa (IC 50 : 0.032 nM) Aiyar, N. et al. (1996) J. Biol. Chem., 271: 11325-11329. specific binding (% of control) 100 50 0 -13 - 12 -11 - 10 -9 -8 -7 -6 log [drug] (M) hCGRPα CGRP 8-37 adrenomedullin human calcitonin CGRP cellul ar Ref. 1621 Ref. 1622 Q 3 weeks Agonist effect Antagonist effect Source human recombinant (CHO cells) Measured product cAMP Detection method HTRF Agonist effect Control hCGRPa (10 nM) Reference hCGRPa (EC 50 : 0.11 nM) Antagonist effect Stimulant hCGRPa (0.3 nM) Reference hCGRPa (8-37) (IC 50 : 26 nM) Aiyar, N. et al. (1996) J. Biol. Chem., 271: 11325-11329. cAMP modulation (% of control) 100 50 0 -13 -12 -11 -10 -9 -8 -7 -6 -5 log [agonist] (M) hCGRPα adrenomedullin amylin 100 50 0 -10 -9 -8 -7 -6 -5 log [antagonist] (M) hCGRPα (8-37) CGRP tissue Ref. 0306 Q 4 weeks Source rat vas deferens (field-stimulated) Agonist hCGRPa (pD 2 = 9) Antagonist hCGRPa (8-37) (pA 2 = 6.3) Test concentrations 3 concentrations, n=2 (2 tissues) for both activities [Solvent] must be kept ≤ 0.1% Longmore, J. et al. (1994) Eur. J. Pharmacol., 265: 53-59. tension (% of control) -12 -11 -12 -11 -11 -10 -12 -11 100 -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 -11 -10 -9 -8 -7 log [agonist] (M) -9 -8 -7 -6 -5 -4 hCGRPα (8-37) none 1 µM ❚ calcium sensing CaS cellul ar Ref. 2144 Ref. 2146 Q 3 weeks Agonist effect Antagonist effect Source human recombinant (HEK-293 cells) Measured product intracellular [Ca 2+ ] Detection method fluorimetry Agonist effect Control neomycin (100 µM) Reference neomycin (EC 50 : 11 µM) Antagonist effect Stimulant neomycin (30 µM) Reference unavailable Quinn, S.J. et al. (1997) Am. J. Physiol., 273: 1315-1323. Ca 2+ mobilization (% of control) 100 50 0 -7 -6 -5 -4 -3 -2 log [agonist] (M) neomycin gadolinium (III) chloride hexahydrate spermine CaCl2 [Solvent] must be kept ≤ 0.1% antagonist effect: no graph available -11 -10 -9 -8 -7 -6 -5 -4 -10 -9 -8 -7 ❚ For radioligand binding assays, how should I choose between the agonist and the antagonist models when both are -11 -10 -9 -8 -7 -6 -5 -4 available? -12 -11 -10 -9 -8 -7 -6 -5 -4 -3 -12 -11 -10 -9 -8 -7 For some binding assays two models are available using either agonist or antagonist as radioligand. -12 -11 -10 -9 -8 -7 -6 -5 G-protein-coupled receptors have both high-affinity and low-affinity states that are bound differently by agonists and antagonists. Whereas -10 -9 -8 -7 -6 -5 -4 the antagonists bind with an equal affinity to both affinity states, agonists bind poorly to the low affinity state of the receptor. Therefore, it is advisable to use an antagonist radioligand to evaluate the binding of antagonists knowing that this may fail to reveal the binding of agonists. On the other hand, an assay using an agonist radioligand is suitable to evaluate both agonists and antagonists. The testing of a compound in both assays and the comparison of its competition curves against each radioligand may provide information about its functional activity at the receptor. -12 -11
27 ❚ cannabinoid CB 1 - agonist radioligand binding Ref. 0036 Q 3 weeks Included in: ExpresS Profile High-throughput profile Diversity profile BioPrint ® profile Organ safety profile Source Ligand Kd Non specific Reference human recombinant (CHO cells) [ 3 H]CP 55940 (0.5 nM) 3.5 nM WIN 55212-2 (10 µM) CP 55940 (IC 50 : 0.58 nM) specific binding (% of control) 100 50 0 -11 - 10 -9 -8 -7 -6 -5 CP 55940 WIN 55212-2 AM 281 anandamide log [drug] (M) Rinaldi-Carmona, M. et al. (1996) J. Pharmaco. Exp. Ther., 278: 871-878. [CUSTOM OFFER] at cerebellum model (Ref. 0035), please contact us at customresearch@cerep.com Cerep services Receptors [GPCRs] Ion channels CB 1 cellul ar Ref. 1744 Ref. 1745 Q 3 weeks Agonist effect Antagonist effect Source human recombinant (CHO cells) Measured product cAMP Detection method HTRF Agonist effect Control CP 55940 (100 nM) Reference CP 55940 (EC 50 : 0.8 nM) Antagonist effect Stimulant CP 55940 (10 nM) Reference AM 281 (IC 50 : 100 nM) Felder, C.C. et al. (1995) Mol. Pharmacol., 48: 443-450. cAMP modulation (% of control) 100 100 50 50 0 0 -12 -11 -10 -9 -8 -7 -6 -5 -4 -12 -11 -10 -9 -8 -7 -6 -5 log [agonist] (M) log [antagonist] (M) CP 55940 AM 281 WIN 55212-2 AM 251 anandamide AM 630 JWH 133 [Solvent] must be kept ≤ 0.3% Transporters Kinases CB 1 - inverse agonist effect cellul ar Ref. 2378 Q 3 weeks Source Measured product cAMP Detection method HTRF human recombinant (CHO cells) Control AM 281 (3 µM) Reference AM 281 (EC 50 : 33.2 nM) [Solvent] must be kept ≤ 0.3% Ross, R.A. et al. (1999) Brit. J. Pharmacol., 126: 665-672. -12 -11 -11 -10 -12 -11 -12 -11 -9 -8 -7 -6 -5 -4 -10 -9 -8 -7 -10 -9 -8 -7 -10 -9 -8 -7 -6 -5 -9 -8 -7 -6 -5 -10 -4 -11 -10 -9 -8 -7 -6 -5 -4 Epigenetic & DNA-related enzymes Other enzymes CB 1 tissue Ref. 0307 Q 4 weeks Source mouse vas deferens (field-stimulated) Agonist CP 55940 (pD 2 = 8.7) Antagonist AM 281 Test concentrations 3 concentrations, n=2 (2 tissues) for both activities [Solvent] must be kept ≤ 0.1% Rinaldi-Carmona, M. et al. (1994) FEBS Lett., 350: 240-244. tension (% of control) 100 50 0 -9 -7 -6 -10 -8 log [agonist] (M) CP 55940 anandamide Specialized cellular assays Standard profiles CB 2 - agonist radioligand binding Ref. 0037 Q 3 weeks Included in: Diversity profile BioPrint ® profile Organ safety profile Source Ligand Kd Non specific Reference human recombinant (CHO cells) [ 3 H]WIN 55212-2 (0.8 nM) 1.5 nM WIN 55212-2 (5 µM) WIN 55212-2 (IC 50 : 1 nM) Munro, S. et al. (1993) Nature, 365: 61-65. 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 Assay developed in 2010 New assay conditions Human Q Standard turnaround time 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: adykinin ❚ 25 B 2 cellul ar Ref.
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:
79 Cerep services receptors Recept
Page 81 and 82:
81 LXRb - agonist radioligand bindi
Page 83 and 84:
83 Cerep services receptors Recept
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 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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