WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 532050
CAS#: 6508-43-6
Description: L-152,804 is a potent, selective non-peptide neuropeptide Y Y5 receptor antagonist (Ki = 26 nM for hY5). L-152,804 displays > 300-fold selectivity over hY1, hY2, and hY4 receptors.
MedKoo Cat#: 532050
Name: L-152,804
CAS#: 6508-43-6
Chemical Formula: C23H26O4
Exact Mass: 366.1831
Molecular Weight: 366.457
Elemental Analysis: C, 75.38; H, 7.15; O, 17.46
Synonym: L-152,804; L 152,804; L152,804.
IUPAC/Chemical Name: 9-(2-hydroxy-4,4-dimethyl-6-oxo-1-cyclohexenyl)-3,3-dimethyl-4,9-dihydro-2H-xanthen-1-one
InChi Key: CCJIUBMPDVWYLU-UHFFFAOYSA-N
InChi Code: InChI=1S/C23H26O4/c1-22(2)9-14(24)20(15(25)10-22)19-13-7-5-6-8-17(13)27-18-12-23(3,4)11-16(26)21(18)19/h5-8,19,24H,9-12H2,1-4H3
SMILES Code: O=C1C(C(C2=C(O)CC(C)(C)CC2=O)C3=C(C=CC=C3)O4)=C4CC(C)(C)C1
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
| Biological target: | L 152804 is an orally active and selective neuropeptide Y Y5 receptor (NPY5-R) antagonist, with a Ki of 26 nM for hY5. |
| In vitro activity: | TBD |
| In vivo activity: | Intracerebroventricular (i.c.v.) (30 microg) or oral (10 mg/kg) administration of L-152,804 significantly inhibited food intake evoked by i.c.v.-injected bovine pancreatic peptide (bPP, 5 microg; a moderately selective Y4, Y5 agonist) in satiated SD rats. Reference: Biochem Biophys Res Commun. 2000 May 27;272(1):169-73. https://pubmed.ncbi.nlm.nih.gov/10872822/ |
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 80.83 | 220.56 |
The following data is based on the product molecular weight 366.457 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 | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | 1. Kanatani A, Ishihara A, Iwaasa H, Nakamura K, Okamoto O, Hidaka M, Ito J, Fukuroda T, MacNeil DJ, Van der Ploeg LH, Ishii Y, Okabe T, Fukami T, Ihara M. L-152,804: orally active and selective neuropeptide Y Y5 receptor antagonist. Biochem Biophys Res Commun. 2000 May 27;272(1):169-73. doi: 10.1006/bbrc.2000.2696. PMID: 10872822. 2. Long M, Zhou J, Li D, Zheng L, Xu Z, Zhou S. Long-Term Over-Expression of Neuropeptide Y in Hypothalamic Paraventricular Nucleus Contributes to Adipose Tissue Insulin Resistance Partly via the Y5 Receptor. PLoS One. 2015 May 18;10(5):e0126714. doi: 10.1371/journal.pone.0126714. PMID: 25993471; PMCID: PMC4436377. |
| In vitro protocol: | TBD |
| In vivo protocol: | 1. Kanatani A, Ishihara A, Iwaasa H, Nakamura K, Okamoto O, Hidaka M, Ito J, Fukuroda T, MacNeil DJ, Van der Ploeg LH, Ishii Y, Okabe T, Fukami T, Ihara M. L-152,804: orally active and selective neuropeptide Y Y5 receptor antagonist. Biochem Biophys Res Commun. 2000 May 27;272(1):169-73. doi: 10.1006/bbrc.2000.2696. PMID: 10872822. 2. Long M, Zhou J, Li D, Zheng L, Xu Z, Zhou S. Long-Term Over-Expression of Neuropeptide Y in Hypothalamic Paraventricular Nucleus Contributes to Adipose Tissue Insulin Resistance Partly via the Y5 Receptor. PLoS One. 2015 May 18;10(5):e0126714. doi: 10.1371/journal.pone.0126714. PMID: 25993471; PMCID: PMC4436377. |
1: Long M, Zhou J, Li D, Zheng L, Xu Z, Zhou S. Long-Term Over-Expression of Neuropeptide Y in Hypothalamic Paraventricular Nucleus Contributes to Adipose Tissue Insulin Resistance Partly via the Y5 Receptor. PLoS One. 2015 May 18;10(5):e0126714. doi: 10.1371/journal.pone.0126714. PubMed PMID: 25993471; PubMed Central PMCID: PMC4436377.
2: Sørensen G, Wörtwein G, Fink-Jensen A, Woldbye DP. Neuropeptide Y Y5 receptor antagonism causes faster extinction and attenuates reinstatement in cocaine-induced place preference. Pharmacol Biochem Behav. 2013 Apr;105:151-6. doi: 10.1016/j.pbb.2013.02.010. PubMed PMID: 23454535.
3: Sørensen G, Jensen M, Weikop P, Dencker D, Christiansen SH, Loland CJ, Bengtsen CH, Petersen JH, Fink-Jensen A, Wörtwein G, Woldbye DP. Neuropeptide Y Y5 receptor antagonism attenuates cocaine-induced effects in mice. Psychopharmacology (Berl). 2012 Aug;222(4):565-77. doi: 10.1007/s00213-012-2651-y. PubMed PMID: 22367168.
4: Medeiros PJ, Al-Khazraji BK, Novielli NM, Postovit LM, Chambers AF, Jackson DN. Neuropeptide Y stimulates proliferation and migration in the 4T1 breast cancer cell line. Int J Cancer. 2012 Jul 15;131(2):276-86. doi: 10.1002/ijc.26350. PubMed PMID: 21823118.
5: Schroeder JP, Overstreet DH, Hodge CW. The neuropeptide-Y Y5 receptor antagonist L-152,804 decreases alcohol self-administration in inbred alcohol-preferring (iP) rats. Alcohol. 2005 Jul;36(3):179-86. PubMed PMID: 16377459.
6: Woldbye DP, Nanobashvili A, Sørensen AT, Husum H, Bolwig TG, Sørensen G, Ernfors P, Kokaia M. Differential suppression of seizures via Y2 and Y5 neuropeptide Y receptors. Neurobiol Dis. 2005 Dec;20(3):760-72. PubMed PMID: 15979311.
7: Stratford TR, Wirtshafter D. NPY mediates the feeding elicited by muscimol injections into the nucleus accumbens shell. Neuroreport. 2004 Dec 3;15(17):2673-6. PubMed PMID: 15570176.
8: Schroeder JP, Iller KA, Hodge CW. Neuropeptide-Y Y5 receptors modulate the onset and maintenance of operant ethanol self-administration. Alcohol Clin Exp Res. 2003 Dec;27(12):1912-20. PubMed PMID: 14691378.
9: Silva AP, Carvalho AP, Carvalho CM, Malva JO. Functional interaction between neuropeptide Y receptors and modulation of calcium channels in the rat hippocampus. Neuropharmacology. 2003 Feb;44(2):282-92. PubMed PMID: 12623227.
10: Kanatani A, Ishihara A, Iwaasa H, Nakamura K, Okamoto O, Hidaka M, Ito J, Fukuroda T, MacNeil DJ, Van der Ploeg LH, Ishii Y, Okabe T, Fukami T, Ihara M. L-152,804: orally active and selective neuropeptide Y Y5 receptor antagonist. Biochem Biophys Res Commun. 2000 May 27;272(1):169-73. PubMed PMID: 10872822.
