Velneperit
Based on 1 publication(s) in Google Scholar
Velneperit (S-2367) is an orally active neuropeptide Y (NPY) Y5 receptor antagonist that can penetrate the blood-brain barrier. Velneperit inhibits the appetite-stimulating and metabolism-inhibiting effects mediated by NPY. Velneperit selectively improves diet-induced obesity in mice. Velneperit enhances the expression of fear acutely by removing the inhibition of CeA Drd2 neurons. Velneperit can be used for the study of obesity.
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- Pureza: 98.25%
- No. CAS: 342577-38-2
- Fòrmula: C17H24F3N3O3S
- Peso molecular:407.45
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) Velneperit
MoreVer todos los productos específicos de isoformas Neuropeptide Y Receptor
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Actividad biológica
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NPY Y5 receptor |
Velneperit (100 mg/kg, p.o., single dose) achieves high brain Y5 receptor occupancy rates of 80-90% and maintains sustained plasma concentrations at elevated levels for up to 15 hours in mice and rats[1].
Velneperit (100 mg/kg, i.p., single dose) rapidly and acutely enhances the fear expression in mice, providing evidence that NPY5R is the endogenous inhibitory receptor of Drd2 neurons[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MHF model established in C57BL/6J mice, Y5R gene knockout (Y5R KO) mice. Leprdb/db mice (deficient in leptin receptor) and Zucker obese rats (deficient in leptin receptor)[1]
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Dosage:30 and 100 mg/kg
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Administration:Oral administration (p.o.), once daily for 14 days
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Result:Significantly and dose-dependently inhibited weight gain caused by the MHF diet.
Reduced the calorie intake and fat accumulation in mice.
Improved plasma insulin levels, but there is no significant change in blood sugar.
Was ineffective in both normal diet mice and genetically obese mice.
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Animal Model:Conditional Fear Model established in C57BL/6J mice (8-12 weeks)[2]
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Dosage:100 mg/kg
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Administration:Intraperitoneal injection (i.p.), single dose
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Result:Enhanced the expression of fear on the first day and no lasting effect the next day.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 342577-38-2
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Appearance Solid
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Peso molecular 407.45
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Fòrmula C17H24F3N3O3S
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Color White to off-white
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SMILES
FC(F)(F)C1=CN=C(NC([C@H]2CC[C@H](NS(=O)(C(C)(C)C)=O)CC2)=O)C=C1
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Synonyms
S2367
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Transl Psychiatry
Cell-type-specific interrogation of CeA Drd2 neurons to identify targets for pharmacological modulation of fear extinction. [Abstract]2018 Aug 22;8(1):164. PMID: 30135420
Solvente y solubilidad
DMSO : ≥ 30 mg/mL (73.63 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (274 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Ishihara A, et al. A neuropeptide Y Y5 antagonist selectively ameliorates body weight gain and associated parameters in diet-induced obese mice. Proc Natl Acad Sci U S A. 2006 May 2;103(18):7154-8. [Content Brief]
[2]. McCullough KM, et al. Cell-type-specific interrogation of CeA Drd2 neurons to identify targets for pharmacological modulation of fear extinction. Transl Psychiatry. 2018 Aug 22;8(1):164. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4543 mL | 12.2714 mL | 24.5429 mL | 61.3572 mL |
| 5 mM | 0.4909 mL | 2.4543 mL | 4.9086 mL | 12.2714 mL | |
| 10 mM | 0.2454 mL | 1.2271 mL | 2.4543 mL | 6.1357 mL | |
| 15 mM | 0.1636 mL | 0.8181 mL | 1.6362 mL | 4.0905 mL | |
| 20 mM | 0.1227 mL | 0.6136 mL | 1.2271 mL | 3.0679 mL | |
| 25 mM | 0.0982 mL | 0.4909 mL | 0.9817 mL | 2.4543 mL | |
| 30 mM | 0.0818 mL | 0.4090 mL | 0.8181 mL | 2.0452 mL | |
| 40 mM | 0.0614 mL | 0.3068 mL | 0.6136 mL | 1.5339 mL | |
| 50 mM | 0.0491 mL | 0.2454 mL | 0.4909 mL | 1.2271 mL | |
| 60 mM | 0.0409 mL | 0.2045 mL | 0.4090 mL | 1.0226 mL |
Velneperit Related Classifications
HY-14423 Related Classifications
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