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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.25%
- CAS 番号: 342577-38-2
- 分子式: C17H24F3N3O3S
- 分子量:407.45
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 Velneperit
MoreNeuropeptide Y Receptor アイソフォーム固有の製品をすべて表示
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生物活性
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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 |
化学情報
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CAS 番号 342577-38-2
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性状 Solid
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分子量 407.45
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分子式 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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別名
S2367
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
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
溶剤 & 溶解度
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (274 KB)
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- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
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- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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取扱説明書 (2659 KB)
参考文献
[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 関連分類
HY-14423 関連分類
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