Featured New Products
Highlighted products recently added to the Tocris Bioscience range
March 2010
Subtype-selective α4β2 partial agonist
3754 | Varenicline
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.
Related Products: Dihydro-β-erythroidine 5-Iodo-A-85380Potent VEGFR, PDGFRβ and KIT inhibitor
3768 | Sunitinib
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.
Related Products: PD 161570 SU 5402 Ki 8751Potent, selective CB2 agonist
3556 | SER 601
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.
Related Products: AM 630 JTE 907 HU 308Potent and selective P2Y12 antagonist
3321 | AR-C 66096
Blocks ADP-induced inhibition of adenylyl cyclase in vitro (PKB =7.6) and inhibits ADP-induced aggregation of washed human platelets (pIC50 = 8.16).
Related Products: (±)-Clopidogrel MRS 2179 MRS 2365Dual CK1/cdk inhibitor
3610 | (R)-DRF053
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.
Related Products: PF 670462 D 4476 Purvalanol AFebruary 2010
High affinity and selective GPR30 antagonist
3678 | G-15
Ki = 20 nM. Displays no affinity for ERα and ERβ at concentrations up to 10 μM. Inhibits agonist-induced calcium mobilization in vitro (EC50 of ~185 nM) and antagonizes the antidepressive effects of estrogen in vivo.
Related Products: G-1 ICI 182,780 TamoxifenSelective Pim kinase inhibitor
3714 | TCS PIM-1 4a
IC50 values are 24 and 100 nM for Pim-1 and Pim-2 respectively. Displays selectivity over a panel of ~50 other kinases tested. Exhibits cytotoxicity in PC3 prostate carcinoma cells in vitro (IC50 = 17 μM).
Related Products: PIM-1 Inhibitor 2 TCS PIM-1 1Selective mTOR inhibitor
3725 | KU 0063794
IC50 ~10 nM for mTORC1 and mTORC2 respectively. Displays no activity at PI 3-K or 76 other kinases tested. Suppresses cell growth and induces G1 cell cycle arrest in vitro.
Related Products: Compound 401 PI 103 RapamycinPrimes ESCs for differentiation
3741 | Stauprimide
Interacts with NME2 and inhibits its nuclear translocation. Increases the efficiency of directed differentiation of mouse and human embryonic stem cells (ESCs) in vitro.
Potent, collagenase-selective MMP inhibitor
2916 | Ro 32-3555
Ki values are 3.0, 3.4, 4.4, 59, 154 and 527 nM for MMP-1, MMP-13, MMP-8, MMP-9, MMP-2 and MMP-3 respectively. Inhibits cartilage breakdown in vitro and in vivo and displays antiarthritic activity. Orally active.
Related Products: Batimastat Marimastat UK 370106January 2010
PAM of δ-containing GABAA receptors
3679 | DS2
EC50 = 142 nM for α4β3δ receptors. Displays no effects on GABA responses mediated by α4β3γ2 and α1β3γ2 receptors.
Related Products: L-655,708 L-838,417 TB 21007Potent and selective P2X7 antagonist
3701 | A 740003
IC50 values are 18 and 40 nM for rat and human receptors respectively. Displays selectivity over a variety of P2X and P2Y receptors up to a concentration of 100 μM. Reduces nociception in animal models of persistent neuropathic and inflammatory pain.
Related Products: AZ 10606120 GW 791343 Ro 0437626Potent and selective CCR3 antagonist
3650 | SB 328437
IC50 = 4 nM. Displays > 2500-fold selectivity over C5aR, LTD4, CCR7, CXCR1 and CXCR2 receptors. Inhibits eotaxin-, eotaxin-2- and MCP-4-induced Ca2+ mobilization.
Related Products: BMS CCR2 22 RS 504393 UCB 35625Tankyrase inhibitor; inhibits wnt signaling
3748 | XAV 939
IC50 values are 0.011 and 0.004 μM for TNKS1 and TNKS2 respectively. Antagonizes wnt signaling via stimulation of β-catenin degradation and stabilization of axin.
Related Products: PJ 34 DR 2313 NU 1025Selective TRPV4 ligands
3745 | RN 1747 & 3746 | RN 1734
RN 1747 is a selective TRPV4 agonist (EC50 values are 0.77, 4.0 and 4.1 μM for hTRPV4, mTRPV4 and rTRPV4 respectively) that also antagonizes TRPM8 at relevant concentrations (IC50 = 4 μM). RN 1734 is a selective TRPV4 antagonist (IC50 values are 2.3, 5.9 and 3.2 μM for hTRPV4, mTRPV4 and rTRPV4 receptors respectively).
December 2009
Selective ERβ agonist
3366 | WAY 200070
Displays 68-fold selectivity over ERα (EC50 values are 2 and 155 nM for ERβ and ERα respectively). Displays antianxiolytic and antidepressive effects in vivo.
Related Products: PHTPP DPN PPTSelective Rho-kinase (ROCK) inhibitor
3726 | GSK 429286
IC50 values are 14, 780 and 1940 nM for ROCK1, RSK and p70S6K respectively. Reverses adrenalin-induced contraction of the rat aortic ring (IC50 = 190 nM) and causes a dose-dependent decrease in mean arterial blood pressure in spontaneous hypertensive rats. Orally active.
Related Products: Y-27632 Glycyl-H 1152Selective positive allosteric modulator at mGlu4
3707 | VU 0361737
EC50 values are 240 and 110 nM at human and rat receptors respectively. Inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors and displays weak activity at mGlu5 and mGlu8 receptors. Brain penetrant.
Related Products: SIB 1893 MPEP VU 0155041 sodium saltPotent and highly selective GPR30 agonist
3577 | G-1
Ki = 11 nM, EC50 = 2 nM. Displays no activity at ERα and ERβ at concentration up to 10 μM. Inhibits migration of SKBr3 cells and MCF-7 cells in response to chemoattractants (IC50 values are 0.7 and 1.6 nM respectively) in vitro.
Related Products: Tamoxifen citrate ICI 182,780 β-EstradiolPotent DNA-dependent protein kinase inhibitor
3712 | NU 7441
IC50 values are 14, 1700, 5000, >100000 and >100000 nM for DNA-PK, mTOR, PI 3-K, ATM and ATR respectively. Potentiates the effects of radiation, doxorubicin and etoposide in human tumor cell lines in vitro and etoposide in a human tumor xenograft model in vivo.
Related Products: NU 7026 DMNB Compound 401November 2009
Potent and selective CB1 antagonist
3676 | PF 514273
Ki values are 1 and > 10000 nM at CB1 and CB2 receptors respectively. Inhibits food intake in vivo following oral administration.
Related Products: AM 251 LY 320135 O-2050Selective FGFR1 and -3 inhibitor
3044 | PD 173074
IC50 values are 5, 21.5, ~100, 17600 and 19800 nM for FGFR3, FGFR1, VEGFR2, PDGFR and c-Src respectively. Inhibits VEGF- and FGF-induced angiogenesis in the mouse cornea model of angiogenesis.
Related Products: SU 5402 SU 6668Selective D2-like agonist
3680 | Ropinirole
D3 > D2 > D4. Causes biphasic spontaneous locomotor activity and contralateral circling in 6-OHDA-lesioned mice. Displays antiParkinsonian activity.
Related Products: (-)-Quinpirole Bromocriptine (S)-(-)-SulpirideBenzodiazepine site agonist
3655 | Zaleplon
Non-benzodiazepine agent that acts as an agonist at the benzodiazepine site. Displays hypnotic, anxiolytic, myorelaxant and anticonvulsant activity.
Related Products: L-655,708 Zolpidem ZopicloneDual site Src kinase inhibitor
3642 | Src I1
IC50 values are 44 and 88 nM for Src and Lck respectively. Can be used in parallel with PP 1 and PP 2 to inhibit Src family kinases.
Related Products: Piceatannol PP 2 PP 1October 2009
Potent, competitive NPY Y1 antagonist
3242 | BMS 193885
Ki = 3.3 nM, IC50 = 5.9 nM. Displays > 47, > 100, > 160, > 160 and > 160-fold selectivity over σ1, α1, Y2, Y4 and Y5 receptors respectively. Reduces food intake and body weight via central Y1 inhibition and is brain penetrant.
Related Products: BIBO 3304 BIBP 3226 [Leu31,Pro34]-Neuropeptide Y (human, rat)Peptide cleaved from PAR1 upon receptor activation
3554 | Parstatin (mouse)
Cell-permeable peptide cleaved from protease-activated receptor 1 (PAR1) upon receptor activation. Attenuates endothelial cell migration and proliferation (IC50 ~ 20 μM), and induces cell cycle arrest.
Related Products: TFLLR-NH2 TRAP-6 SCH 79797Selective σ1 antagonist
3133 | NE 100
Ki = 0.86 nM. Displays > 55-fold selectivity over σ2 receptors and > 6000-fold selectivity over D1, D2, 5-HT1A, 5-HT2 and PCP receptors. Exhibits reversible binding (Kd = 1.2 nM) and displays antipsychotic activity in vivo. Orally active.
Related Products: BD 1047 (+)-SK&F 10047 PRE-084Reverse transcriptase inhibitor
3666 | Tenofovir
Selectively inhibits HIV reverse transcriptase (RNA-dependent DNA polymerase). Prevents cytotoxicity in SIV-infected C-8166 cells in vitro (IC50 = 1.5 μM). Antiviral agent.
Related Products: Acyclovir DAPTAPotent and selective NPY Y5 antagonist
3432 | S 25585
IC50 values are 5.4, > 1000, > 10 000 and > 10 000 nM at Y5, Y1, Y2 and Y4 receptors respectively. Significantly inhibits NPY-induced feeding but not through blockade of Y5 receptors.
Related Products: L-152,804 [cPP1-7,NPY19-23,Ala31,Aib32,Gln34] - hPancreatic Polypeptide CGP 71683September 2009
Potent, orally active DPP-IV inhibitor
3506 | NVP DPP 728
Ki = 11 nM, IC50 = 14 nM. Displays > 15 000-fold selectivity over DPP-II and a range of proline-cleaving proteases. Exhibits antidiabetic activity in vivo.
Related Products: DPPI 1c K 579Diacyl glycerolacyltransferase 1 (DGAT-1) inhibitor
3587 | A 922500
IC50 values are 7 and 24 nM at human and mouse DGAT-1 respectively. Devoid of activity at DGAT-2, ACAT1 or ACAT2. Induces significant weight loss without altering food intake, and decreases liver and plasma triglyceride levels in vivo. Orally active.
Potent Raf kinase inhibitor
3185 | L-779,450
IC50 = 10 nM. Displays > 7, > 30 and > 70-fold selectivity over p38α, GSK3β and Lck respectively. Suppresses DNA synthesis and induces apoptosis in cells that proliferate in response to Raf-1 and A-Raf but not B-Raf.
Related Products: GW 5074 ZM 336372Selective FAAH inhibitor
3307 | PF 750
IC50 = 16.2 nM. Displays no activity at a range of other serine hydrolases. Selectively inhibits FAAH within the central nervous system. Orally active.
Related Products: JNJ 1661010 MAFP AACOCF3Potent and selective CB2 agonist
3088 | HU 308
Ki values are 22.7 nM and > 10 μM for CB2 and CB1 receptors respectively, EC50 = 5.57 nM. Displays antiallodynic activity in the rat hindpaw incision model of postoperative pain.
Related Products: JTE 907 GP 1a AM 630August 2009
Potent and highly selective EP3 antagonist
3342 | L-798,106
Ki values are 0.3, 916, > 5000 and > 5000 nM at EP3, EP4, EP1 and EP2 respectively. Attenuates sulprostone-induced inhibition of EFS-evoked twitch and contractile responses in vivo.
Related Products: L-161,982 U 46619 MisoprostolOrally active, selective 5-HT6 antagonist
3368 | SB 271046
pKi - 9.02 - 8.92. Increases extracellular glutamate and aspartate in the frontal cortex, and exhibits anticonvulsant activity (EC50 = 0.16 μM).
Related Products: EMD 386088 SB 399885 SB 258585SGK inhibitor
3572 | GSK 650394
IC50 values are 62 and 103 nM for SGK1 and SGK2 respectively. Displays > 30-fold selectivity over Akt and other related kinases. Inhibits androgen-stimulated growth of LNCaP cells, a human prostate carcinoma cell line (IC50 ~ 1 μM).
Related Products: Bicalutamide Fluticasone MifepristonePotent AMPK activator
3336 | A 769662
EC50 = 0.8 μM. Displays selectivity towards β1 subunit-containing heterotrimers. Inhibits fatty acid synthesis (IC50 = 3.2 μM) and decreases plasma glucose and triglyceride levels in vivo.
Related Products: Dorsomorphin AICARGABAA receptor positive allosteric modulator
3597 | Indiplon
Ki = 1.2 - 1.7 nM. Acts at the benzodiazepine site. Displays ~ 10-fold selectivity for α1 subunit-containing receptors. Exhibits sedative, hypnotic, anxiolytic and anticonvulsant activity in vivo and is orally active.
Related Products: (-)-Bicuculline methochloride L-655,708 SR 95531July 2009
Functionally selective M1 agonist
3569 | Xanomeline
EC50 values are 0.3, 5, 42, 52 and 92.5 nM at M1, M3, M5, M4 and M2 receptors respectively. Exhibits antipsychotic activity, and improves cognitive deficits and behavioural disturbances in Alzheimer's disease and schizophrenia.
Related Products: Pirenzepine Anti-M1 OxotremorinePotent and selective amylin receptor antagonist
3419 | AC 187
IC50 = 0.48 nM. Displays 38-fold and 400-fold selectivity over calcitonin and CGRP receptors respectively. Increases glucagon secretion, accelerates gastric emptying, alters plasma glucose levels and increases food intake in vivo.
Related Products: CGRP 8-37 (rat) CGRP (rat) α-CGRP (human)Potent and selective GlyT1 inhibitor
3397 | LY 2365109
IC50 values are 15.8 and > 30 000 nM at GlyT1 and GlyT2 respectively. Induces a dose-dependent elevation in CSF levels of glycine, and enhances acetylcholine and dopamine release in the striatum and prefrontal cortex respectively. Produces profound locomotor and respiratory impairments at higher doses.
Related Products: ALX 5407 NFPS SarcosinePotent FGFR and VEGFR inhibitor
3300 | SU 5402
IC50 values are 0.02, 0.03, 0.51 and > 100 μM at VEGFR2, FGFR1, PDGFRβ and EGFR respectively. Inhibits embryonic left-right determination and exhibits potent anticancer activity in vitro and in vivo.
Related Products: SU 6668 SU 5416 ZM 323881P2X7 allosteric modulator
3385 | GW 791343
Exhibits species-specific activity; acts as a negative allosteric modulator of human P2X7 (pIC50 = 6.9 - 7.2) and a positive allosteric modulator of rat P2X7.
Related Products: A 438079 Ro 0437626 AZ 10606120June 2009
Potent and selective PAR2 agonist
3369 | AC 55541
pEC50 = 6.7). Displays no activity at other PAR subtypes. Stimulates cell proliferation, PI hydrolysis and Ca2+ mobilization in vitro (pEC50 values are 6.7, 5.9 and 6.6 respectively) and exhibits pronociceptive activity in vivo.
Related Products: SLIGRL-NH2 SCH 79797 TFLLR-NH2Selective, non-competitive AMPA antagonist
2932 | CP 465022
IC50 = 25 nM in rat cortical neurons. Displays potent anticonvulsant activity. Also significantly blocks the persistent component of Nav1.6 channel activity. Brain penetrant and orally active.
Related Products: GYKI 52466 (S)-AMPA GYKI 47261Potent, broad spectrum MMP inhibitor
2961 | Batimastat
C50 values are 3, 4, 4, 6 and 20 nM for MMP -1, -2, -9, -7 and -3 respectively). Exhibits antiproliferative, anti-invasive and antimetastatic activity in human ovarian carcinoma xenografts in vivo.
Related Products: Marimastat ONO 4817 PD 166793Potent and selective ATM kinase inhibitor
3544 | KU 55933
Ki = 2.2 nM, IC50 values are 13, 2500, 9300, 16600, >100000 and > 100000 nM at ATM, DNA-PK, mTOR, PI 3-K, PI 4-K and ATR respectively. Decreases viability of MCF-7, A549 and HCT116 cells and decreases p21CIP1 levels in vitro.
Related Products: CGK 733 Mirin NSC 109555Potent ErbB receptor family inhibitor
3352 | JNJ 28871063
IC50 values are 21, 22 and 38 nM for ErbB4, EGFR and ErbB2 respectively). Displays potent growth inhibition of human cancer cell lines overexpressing ErbB2 in vitro (IC50.
Related Products: Iressa AG 490 PD 198306May 2009
Potent, selective mGlu5 antagonist
2921 | MTEP hydrochloride
IC50 = 5 nM in Ca2+-flux assay; Ki= 16 nM. Displays anxiolytic activity in vivo and is orally active.
Related Products: MPEP CDPPB CHPGAntiangiogenic. Heparanase inhibitor
2710 | OGT 2115
IC50 = 0.4 μM). Displays no major inhibition of human cytochrome P450 isoenzymes (IC50 > 30 μM). Exhibits antiangiogenic properties in vitro (IC50 = 1 μM).
Related Products: Heparin sodium saltVoltage-independent, CFTR channel blocker
3430 | CFTRinh 172
Ki = 300 nM. Blocks intestinal fluid secretion induced by cholera toxin and Escherichia coli and suppresses cyst growth in animal models of polycystic kidney disease. Orally active.
Related Products: Chromanol 293B Lonidamine GlibenclamidePotent and selective CK1ε and CK1δ inhibitor
3316 | PF 670462
IC50 values are 7.7 and 14 nM for CK1ε and CK1δ respectively. Displays > 30 fold selectivity over 42 other common kinases. Attenuates methamphetamine-stimulated locomotion in vivo.
Related Products: D 4476 Anti-CK1 delta Anti-CK1 epsilonPotent P2X7 receptor antagonist
3323 | AZ 10606120
KD values are 1.4 and 19 nM at human and rat P2X7 receptors respectively. Binds in a positive cooperative manner to sites distinct from, but coupled to, the ATP binding site and acts as a negative allosteric modulator.
Related Products: BzATP A 438079 KN-62April 2009
Selective protein kinase D inhibitor
3327 | CID 755673
IC50 values are 0.182, 0.280, 0.227, >10, 15.3, 20.3, 40.5 and >50 μM at PKD1, PKD2, PKD3, PKC, CAK, PLK1, CAMKIIα and Akt respectively. Inhibits prostate cancer cell proliferation, migration and invasion in vitro.
Related Products: GF 109203X R 59-022 Phorbol 12-myristate 13-acetateSelective mGlu1 antagonist
3060 | A 841720
Displays 34-fold selectivity over mGlu5m (IC50 values are 10 and 342 nM respectively). Exhibits analgesic effects; decreases mechanical allodynia in models of neuropathic pain. Also impairs cognitive function.
Related Products: CDPPB LY 456236 YM 298198Potent and selective α7 nAChR agonist
3092 | PHA 543613
Displays selectivity over α3β4, α1β1γδ, α4β2 and 5-HT3 receptors. Positively influences sensory gating and memory in in vivo models of schizophrenia. Orally active and brain penetrant.
Related Products: PNU 282987 α-Conotoxin ImI NS 1738Potent and selective γ-secretase inhibitor
2627 | L-685,458
IC50 = 17 nM. Displays > 50-fold selectivity over a range of aspartyl, serine and cysteine proteases. Exhibits equal potency for inhibition of Aβ40 and Aβ42 peptides (IC50 values are 48 and 67 nM respectively in human neuroblastoma cells).
Related Products: Compound W JLK 6 DAPTPotent and selective OX2 antagonist
3371 | TCS OX2 29
IC50 = 40 nM. Displays > 250 fold selectivity over OX1 and 50 other receptors, ion channels and transporters.
Related Products: [Ala11,D-Leu15]-Orexin B SB 334867 Orexin A (human, rat, mouse)March 2009
Subtype-selective GABAA partial agonist
3250 | L-838,417
Selectively binds to α1, α2, α3 and α5 subunits (Ki values are 0.79, 0.67, 0.67 and 2.25 nM respectively) but displays no efficacy at α1 (α1-sparing). Exhibits non-sedative anxiolytic, antinociceptive and anti-inflammatory activity in vivo.
Related Products: Muscimol SR 95531 (-)-BicucullineNon-steroidal androgen receptor antagonist
3389 | Bicalutamide
IC50 = 190 nM. Displays peripheral selectivity and does not effect serum levels of LH and testosterone. Exhibits potent anticancer activity in vivo.
Related Products: Nilutamide TestosteronePotent aromatase (CYP19) inhibitor
3388 | Anastrozole
IC50 = 15nM. Displays no discernible effect on adrenocorticoid hormone synthesis. Reduces plasma estrogen levels and exhibits antitumor activity in vivo. Orally active.
Related Products: YM 511 ICI 182,780 PPTJAK2, FLT3 and TrkA inhibitor
3395 | Lestaurtinib
IC50 values are 0.9, 3 and > 25 nM for JAK2, FLT3 and TrkA respectively. Prevents STAT5 phosphorylation (IC50 = 20 - 30 nM). Exhibits antiproliferative activity in vitro and is effective against myeloproliferative disorders in vivo.
Related Products: Cucurbitacin I GW 441756 ZM 449829Potent, selective p38α and p38β inhibitor
2999 | RWJ 67657
IC50 values are 1 and 11 μM for p38α and p38β respectively. Displays no activity at p38γ, p38δ and a range of other kinases. Exhibits cardioprotective and anti-inflammatory activity in vivo. Orally active.
Related Products: SB 203580 JX 401 SD 169February 2009
Positive allosteric modulator at mGlu5
3235 | CDPPB
EC50 values are 10 and 20 nM for human and rat receptors respectively. Antipsychotic; reverses amphetamine-induced locomotor activity and amphetamine-induced deficits in prepulse inhibition in rats.
Related Products: VU 0155041 LY 354740 MMPIPSelective GABAB positive allosteric modulator
3313 | rac BHFF
Increases the potency and efficacy of GABA ( > 15-fold and > 149% respectively). Exhibits anxiolytic activity in vivo and is orally active.
Related Products: CGP 7930 GS 39783 CGP 55845Potent Chk1 inhibitor
3038 | TCS 2312
Ki = 0.38 nM, EC50 = 60 nM. Enhances the cell killing activity of Gemcitabine (Cat. No. 3259) in breast and prostate cancer cell lines and displays antiproliferative effects in vitro.
Related Products: SB 218078 PD 407824 MirinHighly selective CXCR4 antagonist
3299 | AMD 3100
IC50 values are 0.02 - 0.13 and > 25 μM for CXCR4 and all other chemokine receptors respectively. Switches inflammatory responses from Th2 to Th1 type and reduces airway hyperresponsiveness in a mouse model of asthma.
Related Products: BMS CCR2 22 SB 265610 ZK 756326Selective Pim-1 kinase inhibitor
2979 | TCS PIM-1 1
IC50 values are 50, > 20000 and > 20000 nM for Pim-1, Pim-2 and MEK1/2 respectively.
Related Products: NSC 95397 NSC 663284January 2009
Dual cdc7/cdk9 inhibitor
3140 | PHA 767491
IC50 values are 10 and 34 nM respectively. Prevents inititaion of DNA replication and inhibits cell proliferation in a variety of human cell lines (IC50 ~ 0.86 - 5.87 µM).
Related Products: 5-Iodo-A-85380 Ryuvidine SU 9516Selective P2X1 antagonist
2188 | Ro 0437626
IC50 = 3 μM. Displays > 30-fold selectivity over P2X2, P2X3 and P22/3 receptors (IC50 > 100 μM).
Related Products: RO-3 Spinorphin A 438079Microtubule depolymerization agent
3101 | XRP44X
Ras-Net (Elk-3) pathway inhibitor (IC50 = 10-20 nM). Indirectly inhibits Net phosphorylation upstream of Erk1/2 activation. Inhibits angiogenesis and acts as a microtubule depolymerizing agent in vitro.
Related Products: Combretastatin A4 Flutax 1 D-64131Potent aromatase (CYP19) inhibitor
3278 | YM 511
IC50 values are 0.4 and 0.12 nM at rat ovary and human placenta cells respectively. Only weakly inhibits the synthesis of other steroid hormones. Reduces plasma estrogen levels into ranges induced by ovariectomy.
Related Products: Testosterone Nilutamide MetyraponePotent non-competitive NMDA receptor antagonist
3125 | Conantokin-R
IC50 = 93 nM. Suggested to have NR2 subunit selectivity. Exhibits broad anticonvulsant and antiparkinsonian activity in vivo at doses devoid of behavioral toxicity.
Related Products: Conantokin-T Co 101244 D-AP5December 2008
mGlu2 positive allosteric modulator
3283 | LY 487379
Potentiates glutamate-stimulated [35S]GTPγS binding (EC50 values are 1.7 and > 10 μM for mGlu2 and mGlu3 receptors respectively). Devoid of any activity at mGlu5 and mGlu7 receptors.
Related Products: LY 379268 LY 354740 LY 341495Potent and selective CRF1 antagonist
3212 | CP 376395
Ki values are 12 and >10000 nM for CRF1 and CRF2 receptors respectively. Attenuates CRF-induced activation of the HPA axis in vivo following i.v. administration. Orally active.
Related Products: NBI 27914 CP 154526 CRF (human, rat)Potent and selective FAK inhibitor
3239 | PF 573228
IC50 = 4 nM. Displays 50-250-fold selectivity over other protein kinases. Blocks serum and fibronectin-directed migration and decreases focal adhesion turnover in vitro.
Related Products: LY 294002 Y-27632 MarimastatHighly selective NPY Y1 receptor antagonist
2412 | BIBO 3304
IC50 values are 0.38 and 0.72 nM at human and rat receptors respectively. Displays > 2600-fold selectivity over Y2, Y4 and Y5 receptors. Inhibits NPY- and fasting-induced feeding in vivo following central administration.
Related Products: BIIE 0246 Neuropeptide Y (human, rat) [cPP1-7,NPY19-23,Ala31,Aib32,Gln34] -hPancreatic PolypeptidePotent, positive allosteric mGlu4 agonist
3248 | VU 0155041
EC50 = 798 and 693 nM at human and rat mGlu4 receptors respectively. Active in in vivo models of Parkinson's disease following i.c.v. administration.
Related Products: (S)-3,4-DCPG AMN 082 MMPIPNovember 2008
Highly selective group II mGlu agonist
3246 | LY 354740
EC50 values are 5.1 and 24.3 nM at mGlu2 and mGlu3 receptors respectively. Displays antianxiety and antiaddictive activity in vivo. Orally active.
Related Products: LY 379268 LY 341495 DCG IVSelective 5-HT4 partial agonist
3089 | CJ 033466
Displays > 1000-fold selectivity for 5-HT4 over other 5-HT and D2 receptors. Exhibits gastroprokinetic effects in vivo following oral administration.
Related Products: RS 67333 Cisapride MosaprideSelective, reversible FAAH inhibitor
3262 | JNJ 1661010
IC50 = 12nM. Brain penetrant and active in vivo.
Related Products: AACOCF3 LY 2183240 PalmitoylethanolamidePotent TGF-βRI inhibitor
3269 | SD 208
Displays > 100 fold and > 17 fold selectivity over TGF-βRII and other common kinases respectively. Exhibits anti-inflammatory and antitumour activity.
Related Products: A 83-01 D 4476 LY 364947Antiprion agent
3238 | TCS PrP Inhibitor 13
Potently inhibits protease-resistant prion protein (PrP-res) accumulation in two types of prion-infected mouse neuroblastoma (N2a) cell lines (IC50 = 3nM).
October 2008
Selective 5-ht5A antagonist
3188 | SB 699551
pKi values are 8.3 for 5-ht5A and < 6.0 for 5-HT1B/D, 5-HT2A, 5-HT2C, 5-HT1A and 5-HT7 receptors.
Related Products: 5-Carboxamidotryptamine maleateUrotensin II (U-II) receptor antagonist
3162 | [Orn5]-URP
pEC50 = 7.24. Displays no agonist activity unlike other U-II/URP analogues. Inhibits the action of U-II in the rat aorta ring assay.
Related Products: (±)-AC 7954 hydrochloride Urotensin II (human) Urotensin II-related peptidePotent and selective 5-HT6 antagonist
3189 | SB 399885
Displays > 200-fold selectivity for 5-HT6 over other 5-HT receptors (pKi values are 9.11, 8.81 and 9.02 for human recombinant, native rat and native human 5-HT6 receptors respectively).
Related Products: EMD 386088 hydrochloride SB 258585 hydrochloridePotent and selective MC4R agonist
3032 | THIQ
IC50 values are 1.2, 761 and 2067 nM for human MC4R, MC3R and MC1R receptors respectively. Stimulates erectile activity in rats ex copula following systemic administration.
Related Products: HS 024 Melanotan IISelective 5-HT1F agonist
3079 | LY 334370
Ki values are 1.87, 16.4, > 100 (IC50), 176, 189 and 281 (IC50) nM for 5-HT1F, 5-HT1A, 5-HT4, 5-HT1E, 5-HT1B and 5-HT1D receptors respectively. Displays antimigraine effects.
Related Products: LY 344864 hydrochloride BRL 54443September 2008
Selective EGFR inhibitor
3000 | Iressa (Gefitinib)
Shows minimal activity against ErbB-2, KDR, c-flt, PKC, MEK and ERK-2. Blocks EGFR autophosphorylation and inhibits tumour growth in mice bearing a range of human xenografts.
Related Products: AG 1478 PD 158780 AG 490High affinity 5-HT2B antagonist
3077 | LY 272015
Ki values are 0.75, 21.63 and 28.7 nM for 5-HT2B, 5-HT2C and 5-HT2A receptors respectively. Orally active.
Related Products: SB 204741 SB 206553 AltanserinPositive allosteric modulator of α7 nAChR
2995 | NS 1738
Exhibits no substantial activity for α4β2, α3β3 and α1-containing receptors. Displays cognitive-enhancing properties in vivo.
Related Products: PNU 282987 Methyllycaconitine citrate PNU 120596Selective V1b agonist
3127 | d[Leu4,Lys8]-VP
Ki values are 0.16, 64, 100 and 3800 nM for V1b, oxytocin, V2 and V1a receptors respectively. Displays weak antidiuretic, vasopressor and in vitro oxytocic activities.
Related Products: d[Cha4]-AVP SR 49059 [Arg8]-VasopressinPotent and selective inhibitor of iNOS
2866 | BYK 191023
IC50 values are 86, 17000, 162000 nM for iNOS, nNOS and eNOS respectively). Acts in an NADPH- and time-dependent manner. Active in vivo, reverses pathological hypotension in the rodent endotoxin model.
Related Products: AMT L-Canavanine 1400WAugust 2008
Selective EGFR inhibitor
3000 | Iressa (Gefitinib)
Shows minimal activity against ErbB-2, KDR, c-flt, PKC, MEK and ERK-2. Blocks EGFR autophosphorylation and inhibits tumour growth in mice bearing a range of human xenografts.
Related Products: AG 1478 PD 158780 AG 490High affinity 5-HT2B antagonist
3077 | LY 272015
Ki values are 0.75, 21.63 and 28.7 nM for 5-HT2B, 5-HT2C and 5-HT2A receptors respectively. Orally active.
Related Products: SB 204741 SB 206553 AltanserinPositive allosteric modulator of α7 nAChR
2995 | NS 1738
Exhibits no substantial activity for α4β2, α3β3 and α1-containing receptors. Displays cognitive-enhancing properties in vivo.
Related Products: PNU 282987 Methyllycaconitine citrate PNU 120596Selective V1b agonist
3127 | d[Leu4,Lys8]-VP
Ki values are 0.16, 64, 100 and 3800 nM for V1b, oxytocin, V2 and V1a receptors respectively. Displays weak antidiuretic, vasopressor and in vitro oxytocic activities. Related Products: d[Cha4]-AVP SR 49059 [Arg8]-Vasopressin
Potent and selective inhibitor of iNOS
2866 | BYK 191023
IC50 values are 86, 17000, 162000 nM for iNOS, nNOS and eNOS respectively. Acts in an NADPH- and time-dependent manner.
Related Products: AMT L-Canavanine 1400W[top]
Buy Now / Print Quote
Find multiple products by catalog number
New 2009-10 Catalog!
Tocris' new catalog is out now. Packed-full of cutting edge products, request a copy or view PDF today.
Tocris Events
Meet your representative
15 - 18th March, 2010
Manchester, UK
