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| 10mg |
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| Targets |
Velneperit targets the neuropeptide Y (NPY) Y5 receptor. It acts as a potent and selective antagonist at this receptor. The NPY Y5 receptor is involved in the regulation of appetite and energy homeostasis. By antagonizing this receptor, velneperit modulates feeding behavior and has potential applications in obesity treatment.
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| ln Vitro |
In vitro, velneperit is a potent and selective NPY Y5 receptor antagonist. Its activity is assessed by measuring NPY Y5 receptor binding and functional antagonism in cell-based assays. The compound shows selectivity for the Y5 receptor over other NPY receptor subtypes.
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| ln Vivo |
In vivo, velneperit is a once-daily, oral, centrally acting agent. It has been evaluated for the treatment of obesity. It has also been studied for potential therapeutic effects in diabetes, obesity, and cancer. The compound crosses the blood-brain barrier to act on central NPY Y5 receptors.
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| Enzyme Assay |
In vitro receptor binding assays for velneperit measure its affinity for the NPY Y5 receptor using radioligand displacement techniques. Membranes prepared from cells expressing the receptor are incubated with a radiolabeled NPY Y5 ligand and varying concentrations of the compound. Functional assays measure antagonism of NPY-induced signaling.
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| Cell Assay |
In vitro cell-based assays for velneperit use cells expressing NPY Y5 receptors. Cells are treated with serial dilutions of the compound, and NPY Y5 receptor-mediated signaling is measured. The IC50 for inhibition of NPY-induced responses is calculated from dose-response curves. Cell viability is assessed in parallel.
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| Animal Protocol |
In vivo animal models for velneperit include models of obesity and feeding behavior. The compound is administered orally, and its effects on food intake, body weight, and metabolic parameters are evaluated. Pharmacodynamic studies measure NPY Y5 receptor occupancy and modulation of feeding-related pathways.
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| ADME/Pharmacokinetics |
Velneperit has a molecular formula of C₁₇H₂₄F₃N₃O₃S and a molecular weight of 407.45 g/mol. It is soluble in DMSO at ≥30 mg/mL. It is stored at -20°C. It is also known as S-2367 and S2367. The compound is a small molecule neuropeptide Y (NPY) Y5 receptor antagonist.
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| Toxicity/Toxicokinetics |
The toxicity profile of velneperit is characterized in preclinical safety studies. As an NPY Y5 receptor antagonist, the compound is generally well-tolerated at therapeutic doses. The compound is for research use only and is not approved for clinical use. Appropriate safety precautions should be taken during handling.
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| References | |
| Additional Infomation |
Velneperit is an oxygen- and nitrogen-containing organic compound whose function is related to δ-amino acids. Velneperit has been used in clinical trials for the treatment of obesity.
Velneperit (S-2367) is a novel, once-daily, oral, centrally acting small molecule neuropeptide Y (NPY) Y5 receptor antagonist. It has been studied for the treatment of obesity and has potential applications in diabetes and cancer. Velneperit is also known as S-2367 and is intended for laboratory research use only. |
| Molecular Formula |
C17H24F3N3O3S
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|---|---|
| Molecular Weight |
407.45
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| Exact Mass |
407.149
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| CAS # |
342577-38-2
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| PubChem CID |
20629114
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| Appearance |
White to off-white solid powder
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| Density |
1.31
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| LogP |
4.86
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
27
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| Complexity |
618
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
WGEWUYACXPEFPO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H24F3N3O3S/c1-16(2,3)27(25,26)23-13-7-4-11(5-8-13)15(24)22-14-9-6-12(10-21-14)17(18,19)20/h6,9-11,13,23H,4-5,7-8H2,1-3H3,(H,21,22,24)
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| Chemical Name |
4-(tert-butylsulfonylamino)-N-[5-(trifluoromethyl)pyridin-2-yl]cyclohexane-1-carboxamide
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| Synonyms |
S2367; S 2367; S-2367
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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 : ≥ 30 mg/mL (~73.63 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 | 2.4543 mL | 12.2714 mL | 24.5429 mL | |
| 5 mM | 0.4909 mL | 2.4543 mL | 4.9086 mL | |
| 10 mM | 0.2454 mL | 1.2271 mL | 2.4543 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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