Tocris Bioscience - High Performance Life Science Reagents The latest New Products, News and Events from Tocris Bioscience http://www.tocris.com http://www.tocris.com/img/tocris_logo_200.gif Tocris Bioscience | High Performance Life Science Reagents http://www.tocris.com Tocris Bioscience is a leading supplier of innovative, high performance life science research reagents 200 48 Tocris Extends Range of Light-Sensitive Caged Compounds http://www.tocris.com/news/pr-01-03-10.php?utm_campaign=RSS&utm_source=RSS&utm_medium=RSS News 1 1 Mar 2010 11:11 Atipamezole hydrochloride - Selective α antagonist http://tcsrv4/web2009/dispprod.php?ItemId=5428&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 5428
Product: Atipamezole hydrochloride (Cat No. 2937)
Category: Adrenergic Receptors > Adrenergic Alpha-2 Receptors
Biological Activity: Selective α2-adrenergic receptor antagonist (Ki values are 1.1, 1.0, 0.89, 1300 and 6500 nM for α2A, α2B, α2C, α1A and α1B receptors respectively). Brain penetrant. ]]> Adrenergic Receptors New Products 8 Mar 2010 11:48 7-Chlorokynurenic acid sodium salt - Sodium salt of Cat. No. 0237. Potent competitive inhibitor of L-glutamate uptake http://tcsrv4/web2009/dispprod.php?ItemId=238244&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 238244
Product: 7-Chlorokynurenic acid sodium salt (Cat No. 3697)
Category: Neurotransmitter Transporters > Glutamate Transporters
Biological Activity: Sodium salt of Cat.No. 0237, an NMDA receptor antagonist acting at the glycine site. Potent competitive inhibitor of L-glutamate transport into synaptic vesicles. ]]> Neurotransmitter Transporters New Products 11 Feb 2010 14:18 MCH (human, mouse, rat) - Potent endogenous MCH agonist http://tcsrv4/web2009/dispprod.php?ItemId=246142&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 246142
Product: MCH (human, mouse, rat) (Cat No. 3806)
Category: Peptide Receptors > Melanin-concentrating Hormone Receptors
Biological Activity: Potent endogenous agonist at melanin-concentration hormone (MCH) receptors (IC50 values are 0.3 and 1.5 nM and EC50 values are 3.9 and 0.1 nM at MCH1 and MCH2 receptors respectively). Increases food intake in vivo. ]]> Peptide Receptors New Products 8 Mar 2010 14:27 DL-AP4 Sodium salt - Broad spectrum EAA antagonist http://tcsrv4/web2009/dispprod.php?ItemId=238246&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 238246
Product: DL-AP4 Sodium salt (Cat No. 3699)
Category: Glutamate (Ionotropic) Receptors > Non-Selective Ionotropic Glutamate
Biological Activity: Sodium salt of the broad spectrum EAA ligand Cat. No. 0101. See separate isomers (Cat. No's. 0102 and 0103). ]]> Glutamate (Ionotropic) Receptors New Products 12 Feb 2010 16:06 5,7-Dichlorokynurenic acid sodium salt - Sodium salt of Cat. No. 0286. Potent NMDA antagonist, acts glycine site http://tcsrv4/web2009/dispprod.php?ItemId=238245&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 238245
Product: 5,7-Dichlorokynurenic acid sodium salt (Cat No. 3698)
Category: Glutamate (Ionotropic) Receptors > NMDA Receptors
Biological Activity: Sodium salt of Cat. No. 0286, a potent antagonist at the glycine site of the NMDA receptor (Ki = 79 nM vs. [3H]-glycine). ]]> Glutamate (Ionotropic) Receptors New Products 11 Feb 2010 14:24 Theanine - Glutamate receptor ligand http://tcsrv4/web2009/dispprod.php?ItemId=248570&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 248570
Product: Theanine (Cat No. 3847)
Category: Glutamate (Ionotropic) Receptors > Miscellaneous Glutamate
Biological Activity: Amino acid analog of glutamine and component of green tea. Shown to bind to AMPA, Kainate, NMDA and group I mGlu receptors. Displays neuroprotective effects in vivo. Promotes self-renewal of human embryonic stem cells (hESC). ]]> Glutamate (Ionotropic) Receptors New Products 8 Mar 2010 16:39 Acamprosate calcium - GABA agonist and glutamatergic modulator http://tcsrv4/web2009/dispprod.php?ItemId=232274&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 232274
Product: Acamprosate calcium (Cat No. 3618)
Category: GABAA and GABAC Receptors > GABAA Receptors
Biological Activity: GABA receptor agonist and modulator of glutamatergic systems. Reduces alcohol consumption in animal models of alcohol addiction. ]]> GABAA and GABAC Receptors New Products 8 Mar 2010 14:04 Voriconazole - Triazole antifungal agent http://tcsrv4/web2009/dispprod.php?ItemId=243584&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 243584
Product: Voriconazole (Cat No. 3760)
Category: Other Pharmacology > Miscellaneous Compounds
Biological Activity: Triazole antifungal agent. Displays potent activity against Candida, Cryptococcus and Aspergillus species. ]]> Other Pharmacology New Products 4 Mar 2010 14:42 SC 51089 - Selective EP1 receptor antagonist http://tcsrv4/web2009/dispprod.php?ItemId=243578&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 243578
Product: SC 51089 (Cat No. 3758)
Category: 7-TM Receptors > Prostanoid Receptors
Biological Activity: Selective EP1 prostanoid receptor antagonist (Ki values are 1.3, 11.2, 17.5, 61.1, > 100, > 100, > 100, >100 and > 100 μM for EP1, TP, EP3, EP2, EP4, FP and DP receptors respectively). Attenuates PGE2-induced neuronal cell death in vitro and slows tumor growth in vivo. ]]> 7-TM Receptors New Products 16 Feb 2010 15:59 LY 393558 - Dual 5-HT1B/1D antagonist and 5-HT re-uptake inhibitor http://tcsrv4/web2009/dispprod.php?ItemId=219986&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 219986
Product: LY 393558 (Cat No. 3350)
Category: 5-HT1 Receptors > 5-HT1B Receptors
Biological Activity: Dual 5-HT1B/1D receptor antagonist (pKB values are 9.05 and 8.98 respectively) and 5-HT re-uptake inhibitor (pIC50 = 8.48). Potently antagonizes terminal autoreceptor activity in vitro and increases extracellular 5-HT levels above those evoked by fluoxetine in vivo. Also acts as an antagonist at 5-HT2A and 5-HT2B receptors (pKi values are 7.29 and 7.35 respectively). ]]> 5-HT1 Receptors New Products 17 Feb 2010 17:17 Eletriptan hydrobromide - Orally active, selective 5-HT1B/1D agonist http://tcsrv4/web2009/dispprod.php?ItemId=249024&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 249024
Product: Eletriptan hydrobromide (Cat No. 3862)
Category: 5-HT1 Receptors > 5-HT1B Receptors
Biological Activity: Orally active, selective 5-HT1B/1D receptor agonist. Produces a dose-dependent reduction in carotid artery blood flow in vivo. Displays antimigraine activity. ]]> 5-HT1 Receptors New Products 8 Mar 2010 10:54 Sildenafil citrate - Orally active, potent PDE4 inhibitor http://tcsrv4/web2009/dispprod.php?ItemId=243882&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 243882
Product: Sildenafil citrate (Cat No. 3784)
Category: Enzymes > Phosphodiesterases
Biological Activity: Orally active, potent inhibitor of phosphodiesterase 5 (PDE5) (IC50 = 4 nM). Enhances nitric oxide-dependent relaxation of human corpus cavernosum in vitro. ]]> Enzymes New Products 5 Mar 2010 9:46 RS 25344 hydrochloride - Potent PDE4 inhibitor http://tcsrv4/web2009/dispprod.php?ItemId=218554&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 218554
Product: RS 25344 hydrochloride (Cat No. 3315)
Category: Enzymes > Phosphodiesterases
Biological Activity: Potent and selective phosphodiesterase (PDE) 4 inhibitor (IC50 values are 0.28, > 100, 160 and 330 nM at PDE4, PDE1, PDE2 and PDE3 respectively). Inhibits eosinophil chemotaxis and increases progressive motility of spermatozoa in vitro. ]]> Enzymes New Products 12 Feb 2010 12:04 RVD-Hpα - Selective CB1 agonist http://tcsrv4/web2009/dispprod.php?ItemId=243004&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 243004
Product: RVD-Hpα (Cat No. 3744)
Category: Cannabinoid Receptors > CB1 Receptors
Biological Activity: N-terminally extended form of human hemopressin that acts as a selective CB1 receptor agonist. Increases intracellular Ca2+ levels in cells expressing CB1 receptors in vitro. ]]> Cannabinoid Receptors New Products 11 Feb 2010 14:08 Hemopressin (human, mouse) - Selective CB1 inverse agonist http://tcsrv4/web2009/dispprod.php?ItemId=244113&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 244113
Product: Hemopressin (human, mouse) (Cat No. 3791)
Category: Cannabinoid Receptors > CB1 Receptors
Biological Activity: Bioactive endogenous peptide substrate for endopeptidase 24.15 (ep24.15), neurolysin (ep24.16) and ACE. Ki values are 27.76, 3.43 and 1.87 μM respectively. Potent hypotensive in vivo. Also acts as a selective CB1 receptor inverse agonist. Displays antinociceptive activity in vivo. ]]> Cannabinoid Receptors New Products 12 Feb 2010 15:12 SER 601 - Potent, selective CB2 agonist http://tcsrv4/web2009/dispprod.php?ItemId=227235&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 227235
Product: SER 601 (Cat No. 3556)
Category: Cannabinoid Receptors > CB2 Receptors
Biological Activity: Potent and selective CB2 receptor agonist (Ki values are 6.3 nM and 1.2 μM for CB2 and CB1 receptors respectively). Displays analgesic activity in the formalin test in mice. ]]> Cannabinoid Receptors New Products 19 Feb 2010 14:11 Dofetilide - hERG channel blocker; inhibits rapid delayed rectifier K+ current (IKr) http://tcsrv4/web2009/dispprod.php?ItemId=243575&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 243575
Product: Dofetilide (Cat No. 3757)
Category: Potassium Channels > Voltage-Gated Potassium Channels
Biological Activity: Selective potassium channel blocker. Blocks hERG K+ channels; inhibits the rapid delayed-rectifier K+ current (IKr). Displays class III antiarrhythmic properties. ]]> Potassium Channels New Products 1 Mar 2010 11:38 SB 657510 - Selective urotensin-II (UT) receptor antagonist http://tcsrv4/web2009/dispprod.php?ItemId=229458&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 229458
Product: SB 657510 (Cat No. 3571)
Category: Peptide Receptors > Urotensin-II Receptors
Biological Activity: Selective urotensin-II (UT) receptor antagonist (Ki values are 61, 17, 30, 65 and 56 nM at human, monkey, cat, rat and mouse receptors respectively). Inhibits U-II-induced intracellular Ca2+ mobilization (IC50 = 180 nM) and antagonizes the contractile action of U-II in isolated mammalian arteries and aortae (EC50 = 50-189 nM). ]]> Peptide Receptors New Products 25 Feb 2010 14:03 Celecoxib - Selective COX-2 inhibitor http://tcsrv4/web2009/dispprod.php?ItemId=243888&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 243888
Product: Celecoxib (Cat No. 3786)
Category: Oxygenases/Oxidases > Cyclooxygenase
Biological Activity: Selective cyclooxygenase-2 (COX-2) inhibitor (IC50 values are 15 and 0.04 μM for COX-1 and COX-2 respectively). Anti-inflammatory with shorter plasma half-life in vivo than SC 58121 (Cat. No. 2895). Displays chemopreventive activity in in vivo tumor models. ]]> Oxygenases/Oxidases New Products 23 Feb 2010 14:53 BAG 956 - Dual PI 3-kinase and PDK1 inhibitor http://tcsrv4/web2009/dispprod.php?ItemId=231662&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 231662
Product: BAG 956 (Cat No. 3606)
Category: Kinases > PI 3-Kinase
Biological Activity: Dual PDK1 and class I PI3K inhibitor (IC50 values are 245, 56, 446, 35 and 117 nM for PDK1 and PI3K p110 -α, -β, -δ, and -γ respectively). Inhibits cellular AKT phosphorylation at Thr308. Blocks cell proliferation, causing arrest in G1 phase of the cell cycle. Slows tumor progression in mouse xenograft models. ]]> Kinases New Products 9 Mar 2010 11:52 CP 96345 - Potent and selective NK1 antagonist http://tcsrv4/web2009/dispprod.php?ItemId=124227&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 124227
Product: CP 96345 (Cat No. 2893)
Category: Tachykinin Receptors > NK1 Receptor
Biological Activity: Potent and selective non-peptide NK1 receptor antagonist. Attenuates substance P-induced salivary response and inhibits neurogenic inflammation in vivo. ]]> Tachykinin Receptors New Products 18 Feb 2010 11:49 Atorvastatin hemicalcium salt - HMG-CoA reductase inhibitor http://tcsrv4/web2009/dispprod.php?ItemId=243855&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 243855
Product: Atorvastatin hemicalcium salt (Cat No. 3776)
Category: Reductases > HMG-CoA Reductase
Biological Activity: Potent HMG-CoA reductase inhibitor (IC50 = 8 nM). Reduces circulating LDL-C by inhibiting cholesterol biosynthesis and inducing expression of LDL receptors. Inhibits smooth muscle cell proliferation in vitro and exhibits antinociceptive effects in the inflammatory hypernociception model. ]]> Reductases New Products 23 Feb 2010 14:23 Sunitinib malate - Potent VEGFR, PDGFRβ and KIT inhibitor http://tcsrv4/web2009/dispprod.php?ItemId=243827&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 243827
Product: Sunitinib malate (Cat No. 3768)
Category: Receptor Tyrosine Kinases (RTKs) > VEGFR
Biological Activity: Potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor (Ki values are 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT respectively). Also inhibits cellular receptor phosphorylation of FLT3, RET and CSF-1R. Exhibits antiangiogenic and antitumor activity in multiple xenograft models. ]]> Receptor Tyrosine Kinases (RTKs) New Products 1 Mar 2010 11:20 AR-C 66096 tetrasodium salt - Potent and selective P2Y12 antagonist http://tcsrv4/web2009/dispprod.php?ItemId=218812&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 218812
Product: AR-C 66096 tetrasodium salt (Cat No. 3321)
Category: 7-TM Receptors > P2Y Receptors
Biological Activity: Potent and selective P2Y12 receptor antagonist. Blocks ADP-induced inhibition of adenylyl cyclase in vitro (PKB =7.6) and inhibits ADP-induced aggregation of washed human platelets (pIC50 = 8.16). ]]> 7-TM Receptors New Products 12 Feb 2010 15:13 C 021 dihydrochloride - Potent CCR4 antagonist http://tcsrv4/web2009/dispprod.php?ItemId=230171&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 230171
Product: C 021 dihydrochloride (Cat No. 3581)
Category: 7-TM Receptors > Chemokine Receptors
Biological Activity: Potent CCR4 chemokine receptor antagonist (IC50 values are 0.14 and 0.039 μM for inhibition of chemotaxis in human and mouse respectively). ]]> 7-TM Receptors New Products 11 Feb 2010 15:21 Sal 003 - Cell-permeable inhibitor of eIF2α dephosphorylation http://tcsrv4/web2009/dispprod.php?ItemId=236229&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 236229
Product: Sal 003 (Cat No. 3657)
Category: Phosphatases > Protein Ser/Thr Phosphatase
Biological Activity: Cell-permeable inhibitor of cellular phosphatase complexes that dephosphorylate eukaryotic translation initiation factor 2 subunit α (eIF2α). Analog of salubrinal (Cat. No. 2347) with improved aqueous solubility. Shown to prevent the induction of hippocampal long-term potentiation (LTP) and memory formation (LTM) in mice. ]]> Phosphatases New Products 5 Mar 2010 13:40 CP 471474 - Broad spectrum MMP inhibitor http://tcsrv4/web2009/dispprod.php?ItemId=243868&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 243868
Product: CP 471474 (Cat No. 3780)
Category: Proteases > Matrix Metalloprotease
Biological Activity: Broad spectrum matrix metalloprotease (MMP) inhibitor (IC50 values are 0.7, 0.9, 13, 16 and 1170 nM for MMP-2, MMP-13, MMP-9, MMP-3 and MMP-1 respectively). Attenuates early left ventricular dilation after experimental myocardial infarction in mice. ]]> Proteases New Products 16 Feb 2010 15:57 Nelfinavir mesylate - Potent HIV-1 protease inhibitor http://tcsrv4/web2009/dispprod.php?ItemId=243598&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 243598
Product: Nelfinavir mesylate (Cat No. 3766)
Category: Proteases > Other Proteases
Biological Activity: Orally active human immunodeficiency virus protease inhibitor. Potently inhibits HIV-1 protease (Ki = 2 nM) in vitro. ]]> Proteases New Products 19 Feb 2010 9:47 Azithromycin - Antibiotic; inhibits 50S ribosomal subunit formation and elongation at transpeptidation http://tcsrv4/web2009/dispprod.php?ItemId=243838&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 243838
Product: Azithromycin (Cat No. 3771)
Category: Cell Metabolism > DNA, RNA and Protein Synthesis
Biological Activity: Macrolide antibiotic. Inhibits 50S ribosomal subunit formation and elongation at transpeptidation step in gram-positive and gram-negative organisms. Orally active with improved pharmacokinetics over erythromycin in mouse models. ]]> Cell Metabolism New Products 19 Feb 2010 9:38 Linezolid - Antibiotic; inhibits protein synthesis in gram-positive bacteria http://tcsrv4/web2009/dispprod.php?ItemId=243596&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 243596
Product: Linezolid (Cat No. 3765)
Category: Cell Metabolism > DNA, RNA and Protein Synthesis
Biological Activity: Oxazolidinone antibiotic. Inhibits bacterial protein synthesis prior to chain initiation. Displays potent antibacterial activity against a variety of multidrug-resistant gram-positive microbes in vitro and in vivo. ]]> Cell Metabolism New Products 24 Feb 2010 16:35 Trovafloxacin mesylate - Antibiotic; inhibits bacterial DNA synthesis http://tcsrv4/web2009/dispprod.php?ItemId=249025&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 249025
Product: Trovafloxacin mesylate (Cat No. 3863)
Category: Cell Metabolism > DNA, RNA and Protein Synthesis
Biological Activity: Fluoroquinolone antibiotic. Inhibits bacterial DNA topoisomerase IV and DNA gyrase and forms a stable quinolone-DNA complex with these enzymes which reversibly inhibits DNA synthesis. Displays potent activity against gram-positive and gram-negative bacteria. ]]> Cell Metabolism New Products 8 Mar 2010 11:00 Cardamonin - Inhibitor of NF-κB activation; anti-inflammatory http://tcsrv4/web2009/dispprod.php?ItemId=159394&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 159394
Product: Cardamonin (Cat No. 2509)
Category: Cytokine and NF-kB Signaling > NF-kB/IkB
Biological Activity: Chalone analog that display anti-inflammatory activity. Inhibits NO and PGE2 production from LPS- and IFN-γ-induced RAW cells and inhibits TXB2 production via the COX-1 and COX-2 pathways. Inhibits NF-κB activation via inhibition of IκBα degradation and phosphorylation, IκB kinase activation and NF-κB nuclear translocation. ]]> Cytokine and NF-kB Signaling New Products 11 Mar 2010 12:11 (R)-DRF053 dihydrochloride - Dual CK1/cdk inhibitor http://tcsrv4/web2009/dispprod.php?ItemId=232061&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 232061
Product: (R)-DRF053 dihydrochloride (Cat No. 3610)
Category: Kinases > Casein Kinase 1
Biological Activity: Potent, ATP-competitive inhibitor of cyclin-dependent kinase (cdk) and casein kinase 1 (CK1) (IC50 values are 220, 80 and 14 nM for cdk1/cyclin B, cdk5/p25 and CK1 respectively). Selective over GSK-3 α/β (IC50= 4.1 μM). Also shown to inhibit amyloid-β production in N2A-APP695 cells. ]]> Kinases New Products 17 Feb 2010 12:21 Varenicline tartrate - Orally active, subtype-selective α4β2 partial agonist http://tcsrv4/web2009/dispprod.php?ItemId=243507&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 243507
Product: Varenicline tartrate (Cat No. 3754)
Category: Acetylcholine (Nicotinic) Receptors > Nicotinic (a4b2) Receptors
Biological Activity: Orally active, subtype-selective partial agonist at α4β2 nicotinic receptors (Ki values are 0.06, 240, 322 and 3540 nM for α4β2, α3β4, α7, α1βγδ receptors respectively). Reduces nicotine-evoked dopamine release in vitro and decreases nicotine self-administration in vivo. ]]> Acetylcholine (Nicotinic) Receptors New Products 25 Feb 2010 9:58 Pristimerin - Potent, reversible MAGL inhibitor http://tcsrv4/web2009/dispprod.php?ItemId=241264&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 241264
Product: Pristimerin (Cat No. 3731)
Category: Esterases > Lipase
Biological Activity: Potent and reversible inhibitor of monoacylglycerol lipase (MGL) (IC50 = 93 nM). Also suppresses NF-κB activation via inhibition of proteasome chymotrypsin-like activity and IKKα/β. Displays antitumor, anti-inflammatory and antimicrobial activities. ]]> Esterases New Products 11 Mar 2010 15:00 PD 161570 - Selective FGFR inhibitor http://tcsrv4/web2009/dispprod.php?ItemId=241117&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 241117
Product: PD 161570 (Cat No. 3724)
Category: Receptor Tyrosine Kinases (RTKs) > FGFR
Biological Activity: Selective FGFR inhibitor (IC50 values are 40, 262 and 3700 nM for FGFR, PDGFR and EGFR respectively). Inhibits FGFR receptor phosphorylation (IC50 = 622 nM) and growth of A121 cells in vitro. ]]> Receptor Tyrosine Kinases (RTKs) New Products 16 Feb 2010 15:40