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 (21)
Literature

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

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 solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.12 mL 5.58 mL 11.16 mL
5 mM 0.22 mL 1.12 mL 2.23 mL
10 mM 0.11 mL 0.56 mL 1.12 mL
50 mM 0.02 mL 0.11 mL 0.22 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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, supplier, Potent, selective, non-peptide, NPY, Y2, antagonists, Neuropeptide, Y, Receptors, BIIE0246, neuropeptides, NPY, Receptors, Tocris Bioscience

21 Citations for BIIE 0246

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

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

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

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

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

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

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

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

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

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

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

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


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