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
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:
  • Formula:
  • Solubility:
    Soluble to 25 mM in ethanol and to 75 mM in DMSO
  • Purity:
  • Storage:
    Store at +4°C
  • CAS No:
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.
Background References
  1. BIIE0246, a potent and highly selective non-peptide neuropeptide Y Y2 receptor antagonist.
    Dumont et al.
    Br.J.Pharmacol., 2000;129:1075
  2. BIIE0246: a selective and high affinity neuropeptide Y Y2 receptor antagonist.
    Doods et al.
    Eur.J.Pharmacol., 1999;384:R3
  3. Vascular pharmacology of BIIE0246, the first selective non-peptide neuropeptide Y Y2 receptor antagonist, in vivo.
    Br.J.Pharmacol., 2001;133:1073

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

Showing Results 1 - 10 of 21

  1. Activation of Neuropeptide Y Receptors Modulates Retinal Ganglion Cell Physiology and Exerts Neuroprotective Actions In Vitro.
    Authors: Martins Et al.
    ASN Neuro
  2. NPY signaling inhibits extended amygdala CRF neurons to suppress binge alcohol drinking.
    Authors: Pleil Et al.
    Nat Neurosci
  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
  4. Neuropeptide Y stimulates autophagy in hypothalamic neurons.
    Authors: Aveleira Et al.
    Cell Death Dis
  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
  6. Neuropeptide Y receptors activation protects rat retinal neural cells against necrotic and apoptotic cell death induced by glutamate.
    Authors: Santos-Carvalho Et al.
  7. Hypoxia shifts activity of neuropeptide Y in Ewing sarcoma from growth-inhibitory to growth-promoting effects.
    Authors: Tilan Et al.
  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
  9. Stress hormone epinephrine enhances adipogenesis in murine embryonic stem cells by up-regulating the neuropeptide Y system.
    Authors: Han Et al.
    PLoS One
  10. Deconstruction of a neural circuit for hunger.
    Authors: Atasoy Et al.
    Am J Physiol Cell Physiol
  11. Central neuropeptide Y modulates binge-like ethanol drinking in C57BL/6J mice via Y1 and Y2 receptors.
    Authors: Sparrow Et al.
    Cell Metab
  12. 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
  13. 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
  14. Neuropeptide Y inhibits interleukin-1β-induced phagocytosis by microglial cells.
    Authors: Ferreira Et al.
  15. Neuropeptide Y inhibits cholangiocarcinoma cell growth and invasion.
    Authors: Demorrow Et al.
    Iran J Basic Med Sci
  16. 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
  17. Neuropeptide Y fragments derived from neprilysin processing are neuroprotective in a transgenic model of Alzheimer's disease.
    Authors: Rose Et al.
    J Neurosci
  18. Effect of pharmacological manipulations of neuropeptide Y and corticotropin-releasing factor neurotransmission on incubation of conditioned fear.
    Authors: Pickens Et al.
  19. 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
  20. Interaction of NPY compounds with the rat glucocorticoid-induced receptor (GIR) reveals similarity to the NPY-Y2 receptor.
    Authors: Sah Et al.
    J Physiol
  21. Peptide YY3-36 decreases reinstatement of high-fat food seeking during dieting in a rat relapse model.
    Authors: Ghitza Et al.
    J Neurosci
Expand to show all
Tocris Bioscience is the leading supplier of novel and exclusive tools for life science research with over 30 years' experience in the industry. Tocris is a Bio-Techne brand.

Order Details


Contact Information

Molarity Calculator
Calculate the mass, volume or concentration required for a solution

The molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) x Volume (L) x Molecular Weight (g/mol)
An example of a molarity calculation using the molarity calculator:
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?

R&D Systems Guarantee

or select another batch:


Customer Information