| Size | Price | Stock | Qty |
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| 5mg |
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| Targets |
NPY5RA972 targets the neuropeptide Y Y5 receptor (NPY5R), a G-protein-coupled receptor involved in feeding behavior and energy homeostasis. As a selective antagonist, it blocks NPY Y5 receptor-mediated signaling with high potency (IC₅₀ = 3.1 nM) and exceptional selectivity over other NPY receptor subtypes (Y1, Y2, Y4).
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| ln Vitro |
In vitro, NPY5RA972 acts as a potent and selective NPY Y5 receptor antagonist with an IC₅₀ of 3.1 nM for the Y5 receptor. It exhibits >3,000-fold selectivity for Y5 over Y1, Y2, and Y4 receptors. Its in vitro activity is assessed using receptor binding and functional assays to measure antagonism of NPY Y5-mediated signaling.
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| ln Vivo |
NPY5RA-972 (po, 10.5 mg/kg) has a half-life of 6.4 hours, a Tmax value of 1 hour, a Cmax of 35 μM, and a total solution concentration of more than 3 μM/NPY5RA even 24 hours after the notice. It inhibits food intake caused by floating NPY Y5 receptors, but at ad libitum doses of Wistar or meal-modified doses, it has no effect on food intake or body weight [1].
In vivo, NPY5RA972 is orally active and brain penetrant. However, it does not block NPY-induced feeding in vivo. The compound is used in preclinical research to probe NPY Y5-mediated feeding behavior and related CNS pathways. It has been shown to suppress absence seizures in a genetic model through effects on Y5 receptors. |
| Enzyme Assay |
The in vitro receptor binding assay for NPY5RA972 involves measuring its affinity for the NPY Y5 receptor using radioligand binding techniques. These assays use membrane preparations from cells expressing the Y5 receptor and measure the displacement of a labeled ligand by the compound. IC₅₀ values of 3.1 nM for Y5 and >10,000 nM for Y1, Y2, and Y4 are determined.
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| Cell Assay |
In vitro cellular assays for NPY5RA972 are performed using cells expressing the human NPY Y5 receptor. These assays measure the compound's ability to antagonize NPY-induced signaling, such as calcium mobilization or cAMP modulation. The compound's potent and selective Y5 antagonism is demonstrated by its ability to inhibit Y5-mediated effects without affecting Y1, Y2, or Y4 receptors.
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| Animal Protocol |
In vivo animal studies for NPY5RA972 are conducted in rodent models to assess its effects on feeding behavior and CNS function. Studies have shown that the compound does not block NPY-induced feeding in vivo. It has also been evaluated in models of absence seizures, where it suppresses seizures through Y5 receptor-mediated effects.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of NPY5RA972 are characterized by oral activity and central nervous system penetration. As an orally active compound, it achieves sufficient systemic exposure to cross the blood-brain barrier and engage Y5 receptors in the CNS. The compound has a molecular formula of C₂₁H₂₅N₃O₂ and a molecular weight of 351.44 g/mol.
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| Toxicity/Toxicokinetics |
Toxicology studies of NPY5RA972 have been conducted to support its use in preclinical research. As a CNS-penetrant compound, its toxicology profile includes effects on the central nervous system and potential for off-target effects at other NPY receptors or related GPCRs. The compound is for research use only, not for human therapeutic use.
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| References | |
| Additional Infomation |
NPY5RA972 (CAS: 439861-56-0) is a potent, highly selective, orally active, and CNS-penetrant antagonist of the neuropeptide Y Y5 receptor. It has IC₅₀ values of 3.1 nM for Y5 and >10,000 nM for Y1, Y2, and Y4 receptors. The compound has a molecular formula of C₂₁H₂₅N₃O₂ and a molecular weight of 351.44 g/mol. It is for research use only and not for human therapeutic use.
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| Molecular Formula |
C21H25N3O2
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| Molecular Weight |
351.45
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| Exact Mass |
351.195
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| CAS # |
439861-56-0
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| PubChem CID |
9884833
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| Appearance |
White to off-white solid powder
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| LogP |
4.499
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
26
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| Complexity |
506
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ZNFMHLDBJPAFEQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H25N3O2/c1-14(2)24-18-7-5-4-6-16(18)20-15(3)17(8-9-19(20)24)22-21(25)23-10-12-26-13-11-23/h4-9,14H,10-13H2,1-3H3,(H,22,25)
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| Chemical Name |
N-(4-methyl-9-propan-2-ylcarbazol-3-yl)morpholine-4-carboxamide
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| Synonyms |
NPY 5 RA 972; NPY-5-RA-972; NPY5RA972
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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 : ~16.67 mg/mL (~47.43 mM)
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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 | 2.8454 mL | 14.2268 mL | 28.4535 mL | |
| 5 mM | 0.5691 mL | 2.8454 mL | 5.6907 mL | |
| 10 mM | 0.2845 mL | 1.4227 mL | 2.8454 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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