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Submit ReviewL-152,804
Description: Potent, selective non-peptide NPY Y5 receptor antagonist
Chemical Name: 5,5-Dimethyl-2-(2,3,4,9-tetrahydro-3,3-dimethyl-1oxo-1H-xanthen-9-yl)-1,3-cyclohexanedione
Purity: ≥99% (HPLC)
Biological Activity for L-152,804
L-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.
Technical Data for L-152,804
| M. Wt | 366.46 |
| Formula | C23H26O4 |
| Storage | Desiccate at +4°C |
| Purity | ≥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 |
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 for L-152,804
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 36.65 | 100 |
Preparing Stock Solutions for L-152,804
The following data is based on the product molecular weight 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.
| Concentration / Solvent Volume / Mass | 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 |
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Product Datasheets for L-152,804
References for L-152,804
References are publications that support the biological activity of the product.
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
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Keywords: L-152,804, L-152,804 supplier, Potent, selective, non-peptide, NPY, Y5, antagonists, Neuropeptide, Y, Receptors, L152804, neuropeptides, 1382, Tocris Bioscience
9 Citations for L-152,804
Citations are publications that use Tocris products. Selected citations for L-152,804 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
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
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
Ferreira et al (2011) Neuropeptide Y inhibits interleukin-1β-induced phagocytosis by microglial cells. J Biol Chem 8 169 PMID: 22136135
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
Do you know of a great paper that uses L-152,804 from Tocris? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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Peptides Involved in Appetite Modulation Scientific Review
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.