BIIE 0246

Cat. No. 1700

BIIE 0246 C49H57N11O6 [246146-55-4]

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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

Soluble to 25 mM in ethanol and to 75 mM in DMSO
>98 %
Store at +4°C

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.

Certificate of Analysis / Safety Data Sheet

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Malmstrom (2001) Vascular pharmacology of BIIE0246, the first selective non-peptide neuropeptide Y Y2 receptor antagonist, in vivo. Br.J.Pharmacol. 133 1073. PMID: 11487518.

Dumont et al (2000) BIIE0246, a potent and highly selective non-peptide neuropeptide Y Y2 receptor antagonist. Br.J.Pharmacol. 129 1075. PMID: 10725255.

Doods et al (1999) BIIE0246: a selective and high affinity neuropeptide Y Y2 receptor antagonist. Eur.J.Pharmacol. 384 R3. PMID: 10611450.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for BIIE 0246 include:

Alasvand et al (2015) Effect of blockade of neuropeptide Y receptor on aortic intima-media thickness and adipose tissue characteristics in normal and obese mice. J Pharmacol Exp Ther 18 443. PMID: 26124929.

Aveleira et al (2015) Neuropeptide Y stimulates autophagy in hypothalamic neurons. Cell Death Dis 112 E1642. PMID: 25775546.

Martins et al (2015) Activation of Neuropeptide Y Receptors Modulates Retinal Ganglion Cell Physiology and Exerts Neuroprotective Actions In Vitro. ASN Neuro 7. PMID: 26311075.

Pleil et al (2015) NPY signaling inhibits extended amygdala CRF neurons to suppress binge alcohol drinking. Nat Neurosci 18 545. PMID: 25751534.

Panaro et al (2014) The melanocortin-4 receptor is expressed in enteroendocrine L cells and regulates the release of peptide YY and glucagon-like peptide 1 in vivo. J Biol Chem 20 1018. PMID: 25453189.

Reidelberger et al (2013) Role of peptide YY(3-36) in the satiety produced by gastric delivery of macronutrients in rats. Am J Physiol Endocrinol Metab 304 E944. PMID: 23482449.

Santos-Carvalho et al (2013) Neuropeptide Y receptors activation protects rat retinal neural cells against necrotic and apoptotic cell death induced by glutamate. Peptides 4 e636. PMID: 23681231.

Tilan et al (2013) Hypoxia shifts activity of neuropeptide Y in Ewing sarcoma from growth-inhibitory to growth-promoting effects. Oncotarget 4 2487. PMID: 24318733.

Atasoy et al (2012) Deconstruction of a neural circuit for hunger. Am J Physiol Cell Physiol 488 172. PMID: 22801496.

Chen et al (2012) Activation of NPY receptors suppresses excitatory synaptic transmission in a taste-feeding network in the lower brain stem. Am J Physiol Regul Integr Comp Physiol 302 R1401. PMID: 22513746.

Han et al (2012) Stress hormone epinephrine enhances adipogenesis in murine embryonic stem cells by up-regulating the neuropeptide Y system. PLoS One 7 e36609. PMID: 22570731.

Kojima et al (2012) A role for endogenous peptide YY in tachykinin NK(2) receptor-triggered 5-HT release from guinea pig isolated colonic mucosa. Br J Pharmacol 167 1362. PMID: 22758653.

Sparrow et al (2012) Central neuropeptide Y modulates binge-like ethanol drinking in C57BL/6J mice via Y1 and Y2 receptors. Cell Metab 37 1409. PMID: 22218088.

Demorrow et al (2011) Neuropeptide Y inhibits cholangiocarcinoma cell growth and invasion. Iran J Basic Med Sci 300 C1078. PMID: 21270292.

Ferreira et al (2011) Neuropeptide Y inhibits interleukin-1β-induced phagocytosis by microglial cells. Neuropsychopharmacology 8 169. PMID: 22136135.

Ferreira et al (2010) Neuropeptide Y modulation of interleukin-1{β} (IL-1{β})-induced nitric oxide production in microglia. Proc Natl Acad Sci U S A 285 41921. PMID: 20959451.

Pickens et al (2009) Effect of pharmacological manipulations of neuropeptide Y and corticotropin-releasing factor neurotransmission on incubation of conditioned fear. Neuroscience 164 1398. PMID: 19800945.

Rose et al (2009) Neuropeptide Y fragments derived from neprilysin processing are neuroprotective in a transgenic model of Alzheimer's disease. J Neurosci 29 1115. PMID: 19176820.

Ghitza et al (2007) Peptide YY3-36 decreases reinstatement of high-fat food seeking during dieting in a rat relapse model. J Neurosci 27 11522. PMID: 17959795.

Ortiz et al (2007) 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. J Neuroinflammation 323 692. PMID: 17671099.

Sah et al (2007) Interaction of NPY compounds with the rat glucocorticoid-induced receptor (GIR) reveals similarity to the NPY-Y2 receptor. J Physiol 28 302. PMID: 17240481.

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Keywords: BIIE 0246, supplier, Potent, selective, non-peptide, NPY, Y2, antagonists, Neuropeptide, Y, Receptors, BIIE0246, neuropeptides, Tocris Bioscience, NPY Receptor Antagonist products

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