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Submit ReviewL-152,804 is a potent, selective non-peptide neuropeptide Y Y5 receptor antagonist (Ki = 26 nM for hY5). Displays > 300-fold selectivity over hY1, hY2, and hY4 receptors. Causes weight loss in diet-induced obese mice by modulating food intake and energy expenditure. Centrally active upon oral administration in vivo.
分子量 | 366.46 |
公式 | C23H26O4 |
储存 | Desiccate at +4°C |
纯度 | ≥99% (HPLC) |
CAS Number | 6508-43-6 |
PubChem ID | 3765615 |
InChI Key | XQDXIHYKAGHZRX-UHFFFAOYSA-N |
Smiles | CC1(C)CC(=O)C(C2C3=C(OC4=C2C(=O)CC(C)(C)C4)C=CC=C3)C(=O)C1 |
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 36.65 | 100 |
以下数据基于产品分子量 366.46。 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.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.73 mL | 13.64 mL | 27.29 mL |
5 mM | 0.55 mL | 2.73 mL | 5.46 mL |
10 mM | 0.27 mL | 1.36 mL | 2.73 mL |
50 mM | 0.05 mL | 0.27 mL | 0.55 mL |
参考文献是支持产品生物活性的出版物。
Kanatani et al (2000) L-152,804: orally active and selective neuropeptide Y Y5 receptor antagonist. Biochem.Biophys.Res.Commun. 272 169 PMID: 10872822
Mashiko et al (2007) A pair-feeding study reveals that a Y5 antagonist causes weight loss in diet-induced obese mice by modulating food intake and energy expenditure. Mol.Pharmacol. 71 602 PMID: 17105869
Schroeder et al (2005) The neuropeptide-Y Y5 receptor antagonist L-152,804 decreases alcohol self-administration in inbred alcohol-preferring (iP) rats. Alcohol 36 179 PMID: 16377459
If you know of a relevant reference for L-152,804, please let us know.
关键词: L-152,804, L-152,804 supplier, Potent, selective, non-peptide, NPY, Y5, antagonists, Neuropeptide, Y, Receptors, L152804, neuropeptides, 1382, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 L-152,804 的部分引用包括:
Long et al (2015) Long-Term Over-Expression of Neuropeptide Y in Hypothalamic Paraventricular Nucleus Contributes to Adipose Tissue Ins Resistance Partly via the Y5 Receptor. J Pharmacol Exp Ther 10 e0126714 PMID: 25993471
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
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
Ferreira et al (2011) Neuropeptide Y inhibits interleukin-1β-induced phagocytosis by microglial cells. J Biol Chem 8 169 PMID: 22136135
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
Santos-Carvalho et al (2013) Neuropeptide Y receptors activation protects rat retinal neural cells against necrotic and apoptotic cell death induced by glutamate. Neuropsychopharmacology 4 e636 PMID: 23681231
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
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
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.