BIIE 0246

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Cat.No. 1700 - BIIE 0246 | C49H57N11O6 | CAS No. 246146-55-4
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% (HPLC)
Datasheet
Citations (26)
Reviews
Literature (4)

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
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 246146-55-4
PubChem ID 2690
InChI Key MSJODEOZODDVGW-UHFFFAOYSA-N
Smiles O=C(C4=C3C=CC=C4)NC1=CC=CC=C1C3N(CC2)CCN2C(CC5(CCCC5)CC(N[C@@H](CCCNC(N)=N)C(NCCN6C(N(C7=CC=CC=C7)N(C8=CC=CC=C8)C6=O)=O)=O)=O)=O

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
ethanol 23.55 25
DMSO 67.2 75

Preparing Stock Solutions

The following data is based on the product molecular weight 896.06. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.75 mM 1.49 mL 7.44 mL 14.88 mL
3.75 mM 0.3 mL 1.49 mL 2.98 mL
7.5 mM 0.15 mL 0.74 mL 1.49 mL
37.5 mM 0.03 mL 0.15 mL 0.3 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

References are publications that support the biological activity of the product.

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

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

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


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Keywords: BIIE 0246, BIIE 0246 supplier, Potent, selective, non-peptide, NPY, Y2, antagonists, Neuropeptide, Y, Receptors, BIIE0246, neuropeptides, 1700, Tocris Bioscience

26 Citations for BIIE 0246

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

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

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

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

Hao et al (2008) Role of CCK1 and Y2 receptors in activation of hindbrain neurons induced by intragastric administration of bitter taste receptor ligands. Am J Physiol Regul Integr Comp Physiol 294 R33 PMID: 18003792

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

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

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

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

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

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

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

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

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

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

Businaro et al (2018) Platelet Lysate-Derived Neuropeptide y Influences Migration and Angiogenesis of Human Adipose Tissue-Derived Stromal Cells. Sci Rep 8 14365 PMID: 30254326

Chandarana et al (2013) Peripheral activation of the Y2-receptor promotes secretion of GLP-1 and improves glucose tolerance. Mol Metab 2 142 PMID: 24049729

Woldbye et al (2010) Adeno-associated viral vector-induced overexpression of neuropeptide Y Y2 receptors in the hippocampus suppresses seizures. Brain 133 2778 PMID: 20688813

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

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

Herring et al (2012) The cardiac sympathetic co-transmitter galanin reduces acetylcholine release and vagal bradycardia: implications for neural control of cardiac excitability. J Mol Cell Cardiol 52 667 PMID: 22172449

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

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

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


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