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BIIE 0246

Cat. No. 1700 26 篇引用文献 提交评论 说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）

Discontinued Product

This product has been withdrawn from sale and is superseded by BIIE 0246 hydrochloride (Cat. No. 7377)
说明： Potent, selective non-peptide NPY Y2 receptor antagonist
化学名： 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
纯度： ≥98% (HPLC)
说明书
引用文献 (26)
评论
文献 (1)
生物活性 技术数据 说明书 参考文献

生物活性 for BIIE 0246

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.

技术数据 for BIIE 0246

分子量 896.06
公式 C49H57N11O6
储存 Store at +4°C
纯度 ≥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

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

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

产品说明书 for BIIE 0246

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化学品安全技术说明书

参考文献 for BIIE 0246

参考文献是支持产品生物活性的出版物。

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

26 篇 BIIE 0246 的引用文献

引用文献是使用了 Tocris 产品的出版物。 BIIE 0246 的部分引用包括：

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

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

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

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

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

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

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

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

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

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

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

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

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