BIIE 0246

  ( 25 citations )    
Product Datasheet
Catalog Number:1700
Chemical Name:N-[(1S)-4-[(Aminoiminomethyl)amino]-1-[[[2-(3,5-dioxo-1,2-diphenyl-1,2,4-triazolidin-4-yl)ethyl]amino]carbonyl]butyl]-1-[2-[4-(6,11-dihydro-6-oxo-5H-dibenz[b,e]azepin-11-yl)-1-piperazinyl]-2-oxoethyl]-cyclopentaneacetamide
Product Details
Citations (25)
Supplemental Products
Reviews
Biological Activity
Potent, selective and competitive non-peptide antagonist for the neuropeptide Y Y2 receptor (IC50 = 15 nM). Displays > 650-fold selectivity over Y1, Y4 and Y5 receptors. Active in vivo.
Technical Data
  • M.Wt:
    896.06
  • Formula:
    C49H57N11O6
  • Solubility:
    Soluble to 25 mM in ethanol and to 75 mM in DMSO
  • Purity:
    >98
  • Storage:
    Store at +4°C
  • CAS No:
    246146-55-4
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
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Citations:

The citations listed below are publications that use Tocris products. Selected citations for BIIE 0246 include:

25 Citations: Showing 1 - 10
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  1. Activation of Neuropeptide Y Receptors Modulates Retinal Ganglion Cell Physiology and Exerts Neuroprotective Actions In Vitro.
    Authors: Martins Et al.
    ASN Neuro  2015;7
  2. NPY signaling inhibits extended amygdala CRF neurons to suppress binge alcohol drinking.
    Authors: Pleil Et al.
    Nat Neurosci  2015;18:545
  3. Effect of blockade of neuropeptide Y receptor on aortic intima-media thickness and adipose tissue characteristics in normal and obese mice.
    Authors: Alasvand Et al.
    J Pharmacol Exp Ther  2015;18:443
  4. Neuropeptide Y stimulates autophagy in hypothalamic neurons.
    Authors: Aveleira Et al.
    Cell Death Dis  2015;112:E1642
  5. The melanocortin-4 receptor is expressed in enteroendocrine L cells and regulates the release of peptide YY and glucagon-like peptide 1 in vivo.
    Authors: Panaro Et al.
    J Biol Chem  2014;20:1018
  6. Neuropeptide Y receptors activation protects rat retinal neural cells against necrotic and apoptotic cell death induced by glutamate.
    Authors: Santos-Carvalho Et al.
    Peptides  2013;4:e636
  7. Hypoxia shifts activity of neuropeptide Y in Ewing sarcoma from growth-inhibitory to growth-promoting effects.
    Authors: Tilan Et al.
    Oncotarget  2013;4:2487
  8. Role of peptide YY(3-36) in the satiety produced by gastric delivery of macronutrients in rats.
    Authors: Reidelberger Et al.
    Am J Physiol Endocrinol Metab  2013;304:E944
  9. Peripheral activation of the Y2-receptor promotes secretion of GLP-1 and improves glucose tolerance.
    Authors: Chandarana Et al.
    Mol Metab  2013;2:142
  10. Stress hormone epinephrine enhances adipogenesis in murine embryonic stem cells by up-regulating the neuropeptide Y system.
    Authors: Han Et al.
    PLoS One  2012;7:e36609
  11. The cardiac sympathetic co-transmitter galanin reduces acetylcholine release and vagal bradycardia: implications for neural control of cardiac excitability.
    Authors: Herring Et al.
    J Mol Cell Cardiol  2012;52:667
  12. Deconstruction of a neural circuit for hunger.
    Authors: Atasoy Et al.
    Am J Physiol Cell Physiol  2012;488:172
  13. Central neuropeptide Y modulates binge-like ethanol drinking in C57BL/6J mice via Y1 and Y2 receptors.
    Authors: Sparrow Et al.
    Cell Metab  2012;37:1409
  14. Activation of NPY receptors suppresses excitatory synaptic transmission in a taste-feeding network in the lower brain stem.
    Authors: Chen Et al.
    Am J Physiol Regul Integr Comp Physiol  2012;302:R1401
  15. A role for endogenous peptide YY in tachykinin NK(2) receptor-triggered 5-HT release from guinea pig isolated colonic mucosa.
    Authors: Kojima Et al.
    Br J Pharmacol  2012;167:1362
  16. Neuropeptide Y inhibits interleukin-1β-induced phagocytosis by microglial cells.
    Authors: Ferreira Et al.
    Neuropsychopharmacology  2011;8:169
  17. Neuropeptide Y inhibits cholangiocarcinoma cell growth and invasion.
    Authors: Demorrow Et al.
    Iran J Basic Med Sci  2011;300:C1078
  18. Neuropeptide Y modulation of interleukin-1{β} (IL-1{β})-induced nitric oxide production in microglia.
    Authors: Ferreira Et al.
    Proc Natl Acad Sci U S A  2010;285:41921
  19. Adeno-associated viral vector-induced overexpression of neuropeptide Y Y2 receptors in the hippocampus suppresses seizures.
    Authors: Woldbye Et al.
    Brain  2010;133:2778
  20. Neuropeptide Y fragments derived from neprilysin processing are neuroprotective in a transgenic model of Alzheimer's disease.
    Authors: Rose Et al.
    J Neurosci  2009;29:1115
  21. Effect of pharmacological manipulations of neuropeptide Y and corticotropin-releasing factor neurotransmission on incubation of conditioned fear.
    Authors: Pickens Et al.
    Neuroscience  2009;164:1398
  22. Role of CCK1 and Y2 receptors in activation of hindbrain neurons induced by intragastric administration of bitter taste receptor ligands.
    Authors: Hao Et al.
    Am J Physiol Regul Integr Comp Physiol  2008;294:R33
  23. A novel long-acting selective neuropeptide Y2 receptor polyethylene glycol-conjugated peptide agonist reduces food intake and body weight and improves glucose metabolism in rodents.
    Authors: Ortiz Et al.
    J Neuroinflammation  2007;323:692
  24. Interaction of NPY compounds with the rat glucocorticoid-induced receptor (GIR) reveals similarity to the NPY-Y2 receptor.
    Authors: Sah Et al.
    J Physiol  2007;28:302
  25. Peptide YY3-36 decreases reinstatement of high-fat food seeking during dieting in a rat relapse model.
    Authors: Ghitza Et al.
    J Neurosci  2007;27:11522
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VersaClone cDNA Plasmids
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Human NPY2R (NP_000901) VersaClone cDNA

RDC0157
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