L-152,804

Potent, selective non-peptide NPY Y5 receptor antagonist CAS# 6508-43-6

L-152,804

Catalog No. BCC7041----Order now to get a substantial discount!

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Chemical structure

L-152,804

3D structure

Chemical Properties of L-152,804

Cas No. 6508-43-6 SDF Download SDF
PubChem ID 1202745 Appearance Powder
Formula C23H26O4 M.Wt 366.46
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : ≥ 125 mg/mL (341.11 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name (9S)-9-(2-hydroxy-4,4-dimethyl-6-oxocyclohexen-1-yl)-3,3-dimethyl-4,9-dihydro-2H-xanthen-1-one
SMILES CC1(CC(=C(C(=O)C1)C2C3=CC=CC=C3OC4=C2C(=O)CC(C4)(C)C)O)C
Standard InChIKey CCJIUBMPDVWYLU-IBGZPJMESA-N
Standard InChI 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/t19-/m0/s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of L-152,804

DescriptionPotent, 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.

L-152,804 Dilution Calculator

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Preparing Stock Solutions of L-152,804

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.7288 mL 13.6441 mL 27.2881 mL 54.5762 mL 68.2203 mL
5 mM 0.5458 mL 2.7288 mL 5.4576 mL 10.9152 mL 13.6441 mL
10 mM 0.2729 mL 1.3644 mL 2.7288 mL 5.4576 mL 6.822 mL
50 mM 0.0546 mL 0.2729 mL 0.5458 mL 1.0915 mL 1.3644 mL
100 mM 0.0273 mL 0.1364 mL 0.2729 mL 0.5458 mL 0.6822 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on L-152,804

L-152,804: orally active and selective neuropeptide Y Y5 receptor antagonist.[Pubmed:10872822]

Biochem Biophys Res Commun. 2000 May 27;272(1):169-73.

Neuropeptide Y (NPY) elicits food intake through the action of hypothalamic G-protein-coupled receptors. Previous publications indicate that the Y5 receptor may represent one of these postulated hypothalamic "feeding" receptors. Using a potent and orally available Y5 antagonist L-152,804, we evaluated the involvement of the Y5 receptor in feeding regulation. L-152,804 displaced [125I]peptide YY (PYY) binding to human and rat Y5 receptors with Ki values of 26 and 31 nM, respectively, and inhibited NPY (100 nM)-induced increase in intracellular calcium levels via human Y5 receptors (IC50 = 210 nM). L-152,804 did not show significant affinity for human Y1, Y2, and Y4 receptors at a dose of 10 microM. 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. However L-152,804 did not significantly inhibit i.c.v. NPY (5 microg; a Y1, Y2, Y5 agonist)-induced food intake. These findings suggest that L-152,804 is a selective and potent non-peptide Y5 antagonist with oral bioavailability and brain penetrability. In addition, the anorexigenic effects of L-152,804 on bPP-induced feeding revealed participation of the Y5 receptor in feeding regulation, while i.c.v. administration of NPY does not appear to significantly contribute to Y5 stimulated food intake. We conclude that the potent and orally active Y5 antagonist, L-152,804, represents a useful tool to address the physiological role of the Y5 receptor.

The neuropeptide-Y Y5 receptor antagonist L-152,804 decreases alcohol self-administration in inbred alcohol-preferring (iP) rats.[Pubmed:16377459]

Alcohol. 2005 Jul;36(3):179-86.

Neuropeptide-Y (NPY) is the most abundant and widely distributed peptide in the mammalian central nervous system and increases feeding behavior through actions at the Y5 receptor subtype. Recent pharmacological evidence indicates that NPY activity at this receptor subtype can modulate ethanol reinforcement. The purpose of this study was to determine if NPY Y5 receptor antagonism reduces ethanol self-administration and reinforcement in a rodent genetic animal model of alcoholism. Selectively inbred alcohol-preferring (iP) rats were trained to voluntarily consume ethanol (10% vol/vol) versus H2O in a 24-h two-bottle choice test. An additional group of iP rats was trained in operant ethanol self-administration to lever press on a fixed-ratio 1 schedule for ethanol (10% vol/vol) reinforcement. Following establishment of baseline intake or ethanol-reinforced responding, iP rats were injected with L-152,804 (0-20 mg/kg) prior to two-bottle or operant ethanol self-administration sessions. In the two-bottle choice test, L-152,804 (3 and 10 mg/kg, ip) significantly reduced ethanol intake (g/kg) at 4- and 6-h postinjection and had no effect on food intake. In the operant procedure, L-152,804 (10 and 20 mg/kg, ip) significantly reduced both the dosage of self-administered ethanol (g/kg/1-h) and the total number of ethanol-reinforced responses. No effect was observed on latency to the first response or the number of inactive lever presses. These results indicate that blockade of NPY Y5 receptor activity decreases both voluntary ethanol drinking and ethanol reinforcement in a rodent genetic animal model of alcoholism. For this reason, NPY Y5 receptor antagonists may be useful in medical management of alcohol abuse and alcoholism in the human population.

A pair-feeding study reveals that a Y5 antagonist causes weight loss in diet-induced obese mice by modulating food intake and energy expenditure.[Pubmed:17105869]

Mol Pharmacol. 2007 Feb;71(2):602-8.

Neuropeptide Y (NPY) is thought to have a significant role in the physiological control of energy homeostasis. We recently reported that an NPY Y5 antagonist inhibits body weight gain in diet-induced obese (DIO) mice, with a moderate reduction in food intake. To clarify the mechanism of the antiobesity effects of the Y5 antagonist, we conducted a pair-feeding study in DIO mice. The Y5 antagonist at 100 mg/kg produced a moderate feeding suppression leading to an 18% decrease in body weight, without altering body temperature. In contrast, the pair-fed group showed only a transient weight reduction and a reduced body temperature, thus indicating that the Y5 antagonist stimulates thermogenesis. The Y5 antagonist-treated mice showed an up-regulation of uncoupling protein mRNA in brown adipose tissue (BAT) and white adipose tissue (WAT), suggesting that both BAT and WAT contribute to energy expenditure. Thus, the Y5 antagonist induces its antiobesity effects by acting on both energy intake and expenditure.

Description

L 152804 is an orally active and selective neuropeptide Y Y5 receptor (NPY5-R) antagonist, with a Ki of 26 nM for hY5. L 152804 causes weight loss in diet-induced obese mice by modulating food intake and energy expenditure.

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