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BIIE 0246

Catalog #: 1700
26 Citations Datasheet / COA / SDS
Newer Version Available: 7377
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BIIE 0246 | CAS No. 246146-55-4 | NPY Receptor Antagonists
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Description: Potent, selective non-peptide NPY Y2 receptor antagonist

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

Purity: ≥98%

Product Details
Citations (26)
Reviews
Biological Activity Technical Data Background Product Datasheets Calculators

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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. Systemic Central Nervous System (CNS)-targeted Delivery of Neuropeptide Y (NPY) Reduces Neurodegeneration and Increases Neural Precursor Cell Proliferation in a Mouse Model of Alzheimer Disease.
    Spencer B, Potkar R, Metcalf J, Thrin I, Adame A, Rockenstein E, Masliah E
    J Biol Chem, 2016;291(4):1905-20.
  2. Role of peptide YY(3-36) in the satiety produced by gastric delivery of macronutrients in rats.
    Reidelberger, Roger, Haver, Alvin, Chelikani, Prasanth
    Am J Physiol Endocrinol Metab, 2013;304(9):E944-50.
  3. Neuropeptide Y receptor Y5 as an inducible pro-survival factor in neuroblastoma: implications for tumor chemoresistance.
    Czarnecka M, Trinh E, Lu C, Kuan-Celarier A, Galli S, Hong S, Tilan J, Talisman N, Izycka-Swieszewska E, Tsuei J, Yang C, Martin S, Horton M, Christian D, Everhart L, Maheswaran I, Kitlinska J
    Oncogene, 2015;34(24):3131-43.
  4. Interleukin-22 alleviates metabolic disorders and restores mucosal immunity in diabetes.
    Wang, Xiaoting, Ota, Naruhisa, Manzanillo, Paolo, Kates, Lance, Zavala-Solorio, Jose, Eidenschenk, Celine, Zhang, Juan, Lesch, Justin, Lee, Wyne P, Ross, Jed, Diehl, Lauri, van Bruggen, Nicholas, Kolumam, Ganesh, Ouyang, Wenjun
    Nature, 2014;514(7521):237-41.
  5. BIIE0246: a selective and high affinity neuropeptide Y Y2 receptor antagonist.
    Doods et al.
    Eur.J.Pharmacol., 1999;384:R3
  6. BIIE0246, a potent and highly selective non-peptide neuropeptide Y Y2 receptor antagonist.
    Dumont et al.
    Br.J.Pharmacol., 2000;129:1075
  7. Vascular pharmacology of BIIE0246, the first selective non-peptide neuropeptide Y Y2 receptor antagonist, in vivo.
    Malmstrom
    Br.J.Pharmacol., 2001;133:1073

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Citations for BIIE 0246

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

26 Citations: Showing 1 - 10

  1. Platelet Lysate-Derived Neuropeptide y Influences Migration and Angiogenesis of Human Adipose Tissue-Derived Stromal Cells.
    Authors: Businaro Et al.
    Sci Rep  2018;8(1):14365
  2. Activation of Neuropeptide Y Receptors Modulates Retinal Ganglion Cell Physiology and Exerts Neuroprotective Actions In Vitro.
    Authors: Martins Et al.
    ASN Neuro  2015;7
  3. NPY signaling inhibits extended amygdala CRF neurons to suppress binge alcohol drinking.
    Authors: Pleil Et al.
    Nat Neurosci  2015;18:545
  4. 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
  5. Neuropeptide Y stimulates autophagy in hypothalamic neurons.
    Authors: Aveleira Et al.
    Cell Death Dis  2015;112:E1642
  6. 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
  7. 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
  8. Hypoxia shifts activity of neuropeptide Y in Ewing sarcoma from growth-inhibitory to growth-promoting effects.
    Authors: Tilan Et al.
    Oncotarget  2013;4:2487
  9. 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
  10. Peripheral activation of the Y2-receptor promotes secretion of GLP-1 and improves glucose tolerance.
    Authors: Chandarana Et al.
    Mol Metab  2013;2:142
  11. 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
  12. 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
  13. Deconstruction of a neural circuit for hunger.
    Authors: Atasoy Et al.
    Am J Physiol Cell Physiol  2012;488:172
  14. 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
  15. 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
  16. 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
  17. Neuropeptide Y inhibits interleukin-1β-induced phagocytosis by microglial cells.
    Authors: Ferreira Et al.
    Neuropsychopharmacology  2011;8:169
  18. Neuropeptide Y inhibits cholangiocarcinoma cell growth and invasion.
    Authors: Demorrow Et al.
    Iran J Basic Med Sci  2011;300:C1078
  19. 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
  20. Adeno-associated viral vector-induced overexpression of neuropeptide Y Y2 receptors in the hippocampus suppresses seizures.
    Authors: Woldbye Et al.
    Brain  2010;133:2778
  21. 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
  22. 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
  23. 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
  24. 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
  25. 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
  26. 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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