L-152,804

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Cat.No. 1382 - L-152,804 | C23H26O4 | CAS No. 6508-43-6
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)
Datasheet
Citations (7)
Literature

Biological Activity

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.

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Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 36.65 100

Preparing Stock Solutions

The following data is based on the product molecular weight 366.46. 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 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

Safety Datasheet

References

References are publications that support the products' biological activity.

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, supplier, Potent, selective, non-peptide, NPY, Y5, antagonists, Neuropeptide, Y, Receptors, L152804, neuropeptides, NPY, Receptors, Tocris Bioscience

7 Citations for L-152,804

Citations are publications that use Tocris products. Selected citations for L-152,804 include:

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

Ferreira et al (2011) Neuropeptide Y inhibits interleukin-1β-induced phagocytosis by microglial cells. J Biol Chem 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

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

Long et al (2015) Long-Term Over-Expression of Neuropeptide Y in Hypothalamic Paraventricular Nucleus Contributes to Adipose Tissue Insulin 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


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