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| Targets |
NPY-5 receptor antagonist-1 targets the neuropeptide Y5 (NPY-5) receptor, a G protein-coupled receptor (GPCR) involved in appetite regulation and energy homeostasis. As an antagonist, it blocks the receptor from binding its endogenous ligand, neuropeptide Y (NPY), thereby inhibiting downstream signaling pathways. The Ki value of less than 1 microM indicates high affinity for the NPY-5 receptor, making it a valuable tool for studying NPY-mediated physiology.
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| ln Vitro |
NPY-5 receptor antagonist-1 shows high in vitro activity with a Ki value of less than 1 microM at the NPY-5 receptor. This indicates potent competitive binding affinity for the receptor. In functional assays, it would be expected to block NPY-induced signaling, such as calcium mobilization or cAMP inhibition, in NPY-5 expressing cells. The specific IC50 values are not provided, but the Ki suggests submicromolar potency.
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| ln Vivo |
Specific in vivo activity data for NPY-5 receptor antagonist-1 is not provided. As a NPY-5 receptor antagonist, it is used for research on obesity, feeding disorders, and other neurological diseases. In animal models of obesity, NPY-5 antagonists have been shown to reduce food intake, decrease body weight gain, and modulate energy expenditure. The Ki of less than 1 microM suggests that effective concentrations are achievable in vivo.
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| Enzyme Assay |
The binding affinity for NPY-5 receptor is determined by a radioligand binding assay. Procedure: Membranes from CHO cells expressing the human NPY-5 receptor (20 ug protein/well) are incubated with 0.1 nM of a radiolabeled NPY-5 ligand (e.g., [125I]-PYY) in binding buffer (50 mM HEPES, pH 7.4, 10 mM MgCl2, 2 mM CaCl2, 0.5% BSA) for 2 hours at 25degC. Varying concentrations of NPY-5 receptor antagonist-1 (0.001-1000 nM) are added to compete for binding. Non-specific binding is determined with 10 uM unlabeled NPY. Bound radioligand is separated by rapid filtration through GF/B filters and counted. The Ki (< 1 microM) is calculated from the IC50 using the Cheng-Prusoff equation.
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| Cell Assay |
Functional antagonism of the NPY-5 receptor can be assessed using a cAMP accumulation assay, as NPY-5 is Gi-coupled. Procedure: CHO cells expressing the human NPY-5 receptor are seeded in 384-well plates (20,000 cells/well) and pre-incubated with varying concentrations of NPY-5 receptor antagonist-1 (0.1-1000 nM) for 15 minutes. Forskolin (10 microM) is added to elevate baseline cAMP levels, then an EC80 concentration of NPY (10 nM) is added to inhibit cAMP production. After 30 minutes at 37degC, cAMP levels are measured using a homogeneous time-resolved fluorescence (HTRF) cAMP detection kit. The EC50 is calculated as the concentration that blocks 50% of the NPY-induced cAMP inhibition.
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| Animal Protocol |
The in vivo efficacy of NPY-5 receptor antagonist-1 can be evaluated in a mouse model of acute food intake. Procedure: Male C57BL/6J mice (8-10 weeks) are fasted for 18-20 hours with free access to water. NPY-5 receptor antagonist-1 is dissolved in a suitable vehicle (e.g., 10% DMSO, 40% PEG300, 50% saline) and administered orally or intraperitoneally at doses of 1, 3, and 10 mg/kg. Control mice receive vehicle only. Thirty minutes later, NPY (10 ug/kg, intracerebroventricular, ICV) is administered to stimulate feeding. Mice are returned to cages with pre-weighed food pellets. Cumulative food intake is measured at 1, 2, 4, and 6 hours post-NPY injection. A reduction in food intake in treated mice compared to vehicle controls indicates in vivo efficacy of the antagonist.
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| ADME/Pharmacokinetics |
Specific PK data for NPY-5 receptor antagonist-1 is not provided. As a small molecule with a molecular weight of 413.51 g/mol, it is expected to have good oral bioavailability. The Ki value of less than 1 microM suggests that the compound is highly potent, and effective plasma concentrations are likely achievable at moderate doses. The compound is typically stored as a powder at -20degC (3 years) or 4degC (2 years).
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| Toxicity/Toxicokinetics |
Specific toxicology data for NPY-5 receptor antagonist-1 is not available. As an antagonist of the NPY-5 receptor, which is involved in appetite regulation, potential on-target toxicity may include metabolic effects. No specific toxicities are reported in the search results. Standard safety precautions for handling research chemicals should be followed.
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| References | |
| Additional Infomation |
NPY-5 receptor antagonist-1 (Example 57) is a potent antagonist of the neuropeptide Y5 receptor with a Ki of less than 1 microM. NPY is a 36-amino acid neuropeptide that acts through several receptor subtypes (Y1, Y2, Y4, Y5). The Y5 receptor is primarily involved in the central regulation of food intake and energy balance. Antagonists of this receptor have been explored as potential treatments for obesity, feeding disorders, and metabolic syndrome. This compound is for research use only and is not an approved drug.
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| Molecular Formula |
C25H27N5O
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| Molecular Weight |
413.51
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| CAS # |
432506-24-6
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| Appearance |
White to off-white solid powder
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| SMILES |
N1(CC(NC2=CC3C4=C(N(CC)C=3C=C2)C=CC=C4)=O)CCN(C2=NC=CC=C2)CC1
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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 : ~25 mg/mL (~60.46 mM; with ultrasonication)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4183 mL | 12.0916 mL | 24.1832 mL | |
| 5 mM | 0.4837 mL | 2.4183 mL | 4.8366 mL | |
| 10 mM | 0.2418 mL | 1.2092 mL | 2.4183 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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