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 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 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 Repaglinide - KATP channel blocker http://tcsrv4/web2009/dispprod.php?ItemId=246141&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 246141
Product: Repaglinide (Cat No. 3805)
Category: Potassium Channels > Inward rectifier Potassium Channels
Biological Activity: KATP channel blocker that binds with high affinity for SUR1 when co-expressed with Kir6.2 (Kd = 0.42 nM). Antidiabetic glucose regulator with hypoglycaemic effect in vivo. ]]> Potassium Channels New Products 18 Mar 2010 10:47 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 AS 605240 - Potent and selective PI 3-kinase γ (PI3Kγ) inhibitor http://tcsrv4/web2009/dispprod.php?ItemId=230008&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 230008
Product: AS 605240 (Cat No. 3578)
Category: Kinases > PI 3-Kinase
Biological Activity: Potent and selective inhibitor of PI 3-kinase γ (PI3Kγ) (IC50 = 8 nM). Displays 30-fold selectivity over PI3Kδ and PI3Kβ and 7.5-fold selectivity over PI3Kα. Suppresses the progression of joint inflammation and damage in both lymphocyte-independent and lymphocyte-dependent mouse models of rheumatoid arthritis. Orally active and ATP-competitive. ]]> Kinases New Products 17 Mar 2010 11:05 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 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 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 7,8-Dihydroxyflavone - TrkB agonist http://tcsrv4/web2009/dispprod.php?ItemId=247010&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 247010
Product: 7,8-Dihydroxyflavone (Cat No. 3826)
Category: Receptor Tyrosine Kinases (RTKs) > Trk Receptors
Biological Activity: Tyrosine kinase receptor B (TrkB) agonist that binds to the extracellular domain of the receptor (Kd = 320 nM). Inhibits glutamate-triggered apoptosis in hippocampal neurons in vitro and in vivo. ]]> Receptor Tyrosine Kinases (RTKs) New Products 16 Mar 2010 17:58 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 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 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 EHT 1864 - Potent inhibitor of Rac family GTPases http://tcsrv4/web2009/dispprod.php?ItemId=249169&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 249169
Product: EHT 1864 (Cat No. 3872)
Category: Signal Transduction > G Proteins (Small)
Biological Activity: Inhibitor of Rac family GTPases. Blocks activation by direct binding to Rac1, Rac1b, Rac2 and Rac3 (KD values are 40, 50, 60 and 250 nM respectively). Inhibits Rac, Ras and Tiam-induced growth transformation of NIH-3T3 fibroblasts. Reduces β-amyloid peptide production in vivo. ]]> Signal Transduction New Products 12 Mar 2010 15:32 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 6,2',4'-Trimethoxyflavone - Aryl hydrocarbon receptor antagonist http://tcsrv4/web2009/dispprod.php?ItemId=248887&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 248887
Product: 6,2',4'-Trimethoxyflavone (Cat No. 3859)
Category: Nuclear Receptors > Aryl Hydrocarbon Receptor
Biological Activity: Aryl hydrocarbon receptor antagonist (EC50 = 0.9 μM). Exhibits no short term agonist activity and no species or promoter dependence. ]]> Nuclear Receptors New Products 18 Mar 2010 13:21 (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 Losartan potassium - Selective, nonpeptide AT1 antagonist http://tcsrv4/web2009/dispprod.php?ItemId=245560&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 245560
Product: Losartan potassium (Cat No. 3798)
Category: Angiotensin Receptors > Angiotensin AT1 Receptors
Biological Activity: Selective non-peptide angiotensin AT1 receptor antagonist. Inhibits the contractile effects of angiotensin II on rabbit aorta and jugular vein (pA2 = 8.27). Orally active antihypertensive agent. ]]> Angiotensin Receptors New Products 18 Mar 2010 9:51 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 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 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 Rufinamide - Prolongs inactivation of sodium channels; anticonvulsant http://tcsrv4/web2009/dispprod.php?ItemId=247229&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 247229
Product: Rufinamide (Cat No. 3828)
Category: Sodium Channels > Voltage-gated Sodium Channels
Biological Activity: Board spectrum anticonvulsant. Prolongs the inactivation of sodium channels and limits the frequency of action potential firing in cultured and acutely isolated neurons. Displays anticonvulsive activity in a range of animal seizure models. ]]> Sodium Channels New Products 17 Mar 2010 11:37 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 NPY 5RA972 - Potent and selective NPY Y5 antagonist http://tcsrv4/web2009/dispprod.php?ItemId=237570&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 237570
Product: NPY 5RA972 (Cat No. 3677)
Category: Peptide Receptors > NPY Receptors
Biological Activity: Potent and selective neuropeptide Y Y5 receptor antagonist (IC50 values are 3.1, >10000, >10000 and >10000 nM for Y5, Y1, Y2 and Y4 receptors respectively). Does not block NPY-induced feeding in vivo. Orally active and brain penetrant. ]]> Peptide Receptors New Products 18 Mar 2010 9:52 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