| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
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| Targets |
L-152,804 targets the neuropeptide Y Y5 receptor (NPY5-R), a G protein-coupled receptor involved in the regulation of food intake and energy homeostasis. It is a selective, non-peptide antagonist with a Ki of 26 nM for the human Y5 receptor. By blocking Y5 receptor signaling, L-152,804 reduces food intake.
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| ln Vitro |
Relative to hY1, hY2, and hY4 reception, L 152804 exhibits selectivity that is >300 times higher [1].
L-152,804 is a selective NPY5-R antagonist with a Ki of 26 nM for the human Y5 receptor. It is orally active. The compound modulates food intake and energy expenditure. Specific IC50 values for receptor binding are not extensively detailed in standard reference sources. |
| ln Vivo |
L-152,804 causes weight loss in diet-induced obese mice by modulating food intake and energy expenditure. It is orally active. The compound's effects on body weight and metabolic parameters have been demonstrated in vivo.
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| Enzyme Assay |
The binding affinity of L-152,804 to the NPY Y5 receptor can be assessed using radioligand binding assays with membrane preparations from cells expressing recombinant human Y5 receptors. Competition binding experiments are performed with increasing concentrations of L-152,804 against a fixed concentration of a radiolabeled Y5 receptor ligand. Ki values are calculated from competition curves.
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| Cell Assay |
The functional activity of L-152,804 at the NPY Y5 receptor is evaluated in vitro using cells expressing recombinant Y5 receptors. Cells are treated with increasing concentrations of L-152,804, and Y5 receptor-mediated signaling pathways (e.g., calcium mobilization or cAMP modulation) are measured. The compound's antagonist activity is assessed by its ability to block NPY-induced signaling.
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| Animal Protocol |
L-152,804 is administered orally to diet-induced obese mice. The compound is given at various doses via oral gavage. Food intake, body weight, and metabolic parameters (e.g., glucose, insulin, lipid levels) are monitored to assess efficacy.
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| ADME/Pharmacokinetics |
L-152,804 has a molecular formula of C22H26N2O3 and a molecular weight of 366.46. It is orally active. Specific pharmacokinetic parameters such as half-life, bioavailability, and plasma protein binding are not extensively detailed in standard reference sources.
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| Toxicity/Toxicokinetics |
The toxicity profile of L-152,804 is not extensively documented. As an NPY Y5 receptor antagonist, potential adverse effects may include those related to NPY receptor blockade. Specific LD50 values and organ-specific toxicity data are not readily available.
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| References |
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| Additional Infomation |
2-(3,3-dimethyl-1-oxo-4,9-dihydro-2H-xanthon-9-yl)-5,5-dimethylcyclohexane-1,3-dione is one of the xanthones.
L-152,804 (CAS# 6508-43-6) is an orally active and selective neuropeptide Y Y5 receptor (NPY5-R) antagonist with a Ki of 26 nM for the human Y5 receptor. It causes weight loss in diet-induced obese mice by modulating food intake and energy expenditure. The compound is a research tool for studying obesity and metabolism. |
| Molecular Formula |
C23H26O4
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|---|---|
| Molecular Weight |
366.46
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| Exact Mass |
366.183
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| CAS # |
6508-43-6
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| PubChem CID |
3765615
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| Appearance |
White to light yellow solid powder
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| Density |
1.23g/cm3
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| Boiling Point |
506.7ºC at 760 mmHg
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| Flash Point |
173ºC
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| Index of Refraction |
1.603
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| LogP |
4.38
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
27
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| Complexity |
707
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
XQDXIHYKAGHZRX-UHFFFAOYSA-N
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| 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/h5-8,19-20H,9-12H2,1-4H3
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| Chemical Name |
2-(3,3-dimethyl-1-oxo-4,9-dihydro-2H-xanthen-9-yl)-5,5-dimethylcyclohexane-1,3-dione
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| Synonyms |
L152,804; L 152,804; L-152,804
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 125 mg/mL (~341.11 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.68 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.68 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.68 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7288 mL | 13.6441 mL | 27.2881 mL | |
| 5 mM | 0.5458 mL | 2.7288 mL | 5.4576 mL | |
| 10 mM | 0.2729 mL | 1.3644 mL | 2.7288 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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