in vitro PHARMACOLOGY 2011 CATALOG - Cerep

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40 in vitro pharmacology 2011 catalog ❚ glucagon glucagon - agonist radioligand binding Ref. 1407 Q 3 weeks Included in: BioPrint ® profile Source Ligand Kd Non specific Reference human recombinant (CHO cells) [ 125 I]glucagon (0.025 nM) 0.069 nM glucagon (1 µM) glucagon (IC 50 : 1.2 nM) Chicchi, G.G. et al. (1997) J. Biol. Chem., 272: 7765-7769. glucagon cellul ar Ref. 1839 Agonist effect Ref. 1840 Antagonist effect Q 3 weeks Source human recombinant (CHO cells) Measured product cAMP Detection method HTRF Agonist effect Control glucagon (100 nM) Reference glucagon (EC 50 : 0.21 nM) Antagonist effect Stimulant glucagon (1 nM) Reference [des-His 1 -Glu 9 ]-glucagon amide (IC 50 : 2.14 µM) Chichi, G.G. et al. (1997) J. Biol. Chem., 272: 7765-7769. cAMP modulation (% of control) 100 50 0 -12 -11 -10 -9 -8 -7 -6 -5 log [agonist] (M) glucagon GLP-1(7-37) GLP-2(1-34) 100 [Solvent] must be kept ≤ 0.3% 50 0 -9 -8 -7 -6 -5 -4 -3 log [antagonist] (M) [des-His 1 ,Glu 9 ]- glucagon amide L168,049 exendin-3(9-39) secretin cellul ar Ref. 2012 Ref. 2014 Q 3 weeks Agonist effect Antagonist effect Source Measured product cAMP Detection method HTRF human recombinant (CHO cells) Agonist effect Control human secretin (3 nM) Reference human secretin (EC 50 : 0.07 nM) Antagonist effect Stimulant human secretin (0.3 nM) Reference unavailable Ishihara, T. et al. (1991) Embo. J., 10: 1635-1641. -12 -11 -12 -11 -11 -10 -12 -11 -9 -8 -7 -6 -5 -4 -10 -9 -8 -7 -10 -9 -8 -7 -10 -9 -8 -7 -6 -5 -11 -10 -9 -8 -7 -6 -5 -10 -4 [Solvent] must be kept 0.3% -9 -8 -7 -6 -5 -4 -13 -12 -11 -10 -9 -8 -7 -6 -12 -11 -10 -9 -8 -7 -6 -5 -4 ❚ For Glutamate and Glycine assays, see "Other receptors", pp. 86 and 87 ❚ Glycoprotein hormone TSH cellul ar Ref. 2237 Ref. 2239 Q 3 weeks Agonist effect Antagonist effect Source human recombinant (HEK-293 cells) Measured product cAMP Detection method HTRF Agonist effect Control TSH (10 µM) Reference TSH (EC 50 : 27.8 nM) Antagonist effect Stimulant TSH (100 nM) Reference unavailable Rapoport, B. et al. (1998) Endocrinol. Rev., 19: 673-716. [Solvent] must be kept 0.3% ❚ Gonadotrophin-releasing hormone GnRH (LH-RH) - agonist radioligand Source rat pituitary gland Ligand [ 125 I][D-Trp 6 ]-LH-RH (0.05 nM) Kd 0.1 nM Non specific [D-Trp 6 ]-LH-RH (1 µM) binding Reference [D-Trp 6 ]-LH-RH (IC 50 : 0.096 nM) Ref. 0456 Q 4 weeks Halmos, G. et al. (1996) Proc. Natl. Acad. Sci. USA, 93: 2398-2402.
41 ❚ Growth hormone-releasing hormone Cerep services GHRH cellul ar Ref. 2236 Ref. 2238 Q 3 weeks Agonist effect Antagonist effect Source human recombinant (CHO cells) 50 50 Measured product cAMP Detection method HTRF 0 0 Agonist effect Control human GHRF(1-29) (10 nM) Reference human GHRF(1-29) (EC log [agonist] (M) 50 : 0.3 nM) human GHRH(1-29) Antagonist effect Stimulant human GHRF(1-29) (1 nM) GHRF(1-29) glucagon Reference [N-acetyl-Tyr 1 ,D-Arg 2 ]-GHRF secretin (IC 50 : 16 nM) [Solvent] must be kept ≤ 0.3% Gaudreau, P. et al. (1992) J. Med. Chem., 32: 1864-1869. cAMP modulation (% of control) 100 -10 -9 -8 -12 -11 -10 -9 -8 -7 -6 -11 -10 -9 -8 -7 -6 -5 -4 100 log [antagonist] (M) [N-acetyl-Tyr 1 ,D-Arg 2 ]-GHRF JV-1-36 JV-1-38 [des-His 1 -Glu 9 ]-glucagon amide ❚ For Growth factors assays, see "Other receptors", page 87 Receptors [GPCRs] Ion channels ❚ Histamine H 1 - antagonist radioligand binding Ref. 0870 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 (HEK-293 cells) [ 3 H]pyrilamine (1 nM) 1.7 nM pyrilamine (1 µM) pyrilamine (IC 50 : 2.2 nM) Smit, M.J. et al. (1996) Brit. J. Pharmacol., 117: 1071-1080. -12 -11 -12 -11 -12 -11 -10 -9 -8 -7 -10 -9 -8 -7 -10 -9 -8 -7 -6 -5 -9 -8 -7 -6 -5 -10 -4 specific binding (% of control) 100 50 0 -11 -10 -9 -8 -7 -6 -5 -4 -13 -12 -11 -10 -9 -8 -7 -6 log [drug] (M) -12 -11 -10 -9 -8 -7 -6 -5 -4 -11 -10 -9 -8 -7 -6 -5 -4 -3 pyrilamine histamine cimetidine Transporters Kinases Epigenetic & DNA-related enzymes H 1 - antagonist radioligand Source guinea-pig cerebellum Ligand [ 3 H]pyrilamine (0.5 nM) Kd 0.37 nM Non specific triprolidine (100 µM) binding Reference pyrilamine (IC 50 : 0.39 nM) Ref. 0077 Q 3 weeks Dini, S. et al. (1991) Agents and Actions, 33: 181-184. α Other enzymes Specialized cellular assays H 1 cellul ar Ref. 2542 Ref. 2543 Q 3 weeks Included in: Agonist effect Antagonist effect Cellular functional GPCR profile Source human recombinant (HEK-293 cells) Measured product intracellular [Ca 2+ ] Detection method fluorimetry Agonist effect Control histamine (10 µM) Reference histamine (EC 50 : 47 nM) Antagonist effect Stimulant histamine (300 nM) Reference pyrilamine (IC 50 : 5.7 nM) Miller, T.R. et al. (1999) J. Biomol. Screen., 4: 249-258. α [Solvent] must be kept 0.1% Standard profiles Testing conditions H 1 tissue Ref. 0316 Q 4 weeks Source guinea-pig trachea Agonist 2-PEA (pD 2 = 4.9) Antagonist pyrilamine (pA 2 = 9.4) Test concentrations 3 concentrations, n=2 (2 tissues) for both activities [Solvent] must be kept ≤ 0.1% Rappen-Cremer, E. et al. (1989) Agents and Actions, 28: 218-223. tension (% of max.) 100 50 pyrilamine none 1 nM 0 3 nM 10 nM -7 -6 -5 -4 log [agonist] (M) 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: 39 galanin ❚ GAL 2 - agonist radi
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 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
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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