Netupitant
Based on 4 publication(s) in Google Scholar
Netupitant (CID 6451149) is a blood-brain barrier penetrable, orally active NK1 receptor inhibitor with a Ki of 0.95 nM (CHO cells) against the human receptor. Netupitant antagonizes the effects induced by Substance P, inhibits the maximal response of Substance P with a long-lasting action, and suppresses NK1 agonist-induced behaviors in mice and gerbils. Netupitant reduces the frequency of bladder contractions, prolongs contraction intervals, decreases basal pressure at high doses, and acts on the afferent branch of the micturition reflex. Netupitant can be used in research related to overactive bladder, chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, anxiety disorders, and depression.
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 : 99.90%
- CAS 番号: 290297-26-6
- 分子式: C30H32F6N4O
- 分子量:578.59
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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
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 Netupitant
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生物活性
製品説明
IC50 & Target
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hNK1 |
体外実験
Netupitant (1-100 nM; 24 min) potently inhibits Substance P (SP)-induced calcium mobilization in CHO cells expressing human NK1 receptors, exhibiting insurmountable antagonism with a pKB value of 8.87[2].
Netupitant (1 μM; 24 min) acts as a low-potency surmountable antagonist of Substance P-induced calcium mobilization in HEK293 cells expressing the rat NK1 receptor, with a pKB value of 6.57[2].
Netupitant (Compound 21) potently binds to human NK1 receptors expressed in CHO cells, with a Ki value of 0.95 nM, and exhibits at least 100-fold selectivity over NK2 and NK3 receptors[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
Netupitant (0.1-3 mg/kg; intravenous injection; infusion duration 5 min) dose-dependently prolongs the contraction interval without altering the micturition amplitude in anesthetized guinea pigs with acetic acid-induced overactive bladder[1].
Netupitant (1-10 mg/kg, i.p.; single administration) significantly reduces Substance P-induced nociceptive behaviors such as scratching, gnawing and licking in mice[2].
Netupitant (0.3-3 mg/kg; i.p.; single dose; 0.1-3 mg/kg; p.o.; single dose) inhibits GR73632 (HY-P1192)-induced foot-tapping behavior in gerbils[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Dunkin-Hartley (adult female, anesthetized, isovolumetric bladder contraction model)[1]
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Dosage:0.1 mg/kg; 0.3 mg/kg; 1 mg/kg; 3 mg/kg
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Administration:i.v.; infusion over 5 min
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Result:Reduced bladder contraction frequency dose-dependently relative to basal values, with reductions observed at 1 mg/kg and 3 mg/kg.
Showed no effect on bladder contraction amplitude at any tested dose.
Was approximately 3.9 times as potent as L-733,060 in reducing bladder contraction frequency when doses were compared in µmol/kg.
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Animal Model:Dunkin-Hartley (adult female, anesthetized, acetic acid-induced bladder overactivity model)[1]
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Dosage:0.1 mg/kg; 0.3 mg/kg; 1 mg/kg; 3 mg/kg
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Administration:i.v.; infusion over 5 min
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Result:Increased intercontraction interval dose-dependently relative to basal values, with increases observed at all tested doses.
Showed no effect on amplitude of micturition at any tested dose.
Decreased basal pressure at 0.3 mg/kg and 3 mg/kg.
Showed no effect on threshold pressure at any tested dose.
Was approximately 11 times as potent as L-733,060 in increasing intercontraction interval when doses were compared in µmol/kg.
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Animal Model:Swiss mice (male, 20-25 g)[2]
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Dosage:1 mg/kg; 10 mg/kg
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Administration:i.p.; single dose
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Result:Slightly reduced SP-induced nociceptive behavior at 1 mg/kg.
Significantly reduced cumulative SP-induced nociceptive behavior measured over 10 minutes at 10 mg/kg.
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Animal Model:Mongolian gerbils (male and female, 45-65 g)[2]
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Dosage:0.3-3 mg/kg (i.p.); 0.1-3 mg/kg (p.o.)
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Administration:i.p.; single dose; p.o.; single dose
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Result:Dose-dependently inhibited GR73632-induced foot tapping behavior with an ID50 of 1.5 mg/kg when administered intraperitoneally.
Dose-dependently inhibited GR73632-induced foot tapping behavior with an ID50 of 0.5 mg/kg when administered orally.
Fully prevented GR73632-induced foot tapping for 24 hours, reduced the response by approximately 50% at 48 hours, and the response fully recovered by 72 hours when administered orally at 3 mg/kg.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 290297-26-6
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性状 Solid
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分子量 578.59
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分子式 C30H32F6N4O
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Color White to off-white
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SMILES
CN1CCN(C2=CC(C3=C(C)C=CC=C3)=C(N(C)C(C(C4=CC(C(F)(F)F)=CC(C(F)(F)F)=C4)(C)C)=O)C=N2)CC1
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別名
CID 6451149
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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 (4)
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Journal Impact Factor
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Most Recent
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Cell Metab
Cancer cells co-opt nociceptive nerves to thrive in nutrient-poor environments and upon nutrient-starvation therapies. [Abstract]2022 Dec 6;34(12):1999-2017.e10. PMID: 36395769 -
Cancers (Basel)
2024 Nov 12;16(22):3807. PMID: 39594764 -
Exp Neurol
Accelerated onset of the vesicovesical reflex in postnatal NGF-OE mice and the role of neuropeptides. [Abstract]2016 Nov;285(Pt B):110-125. PMID: 27342083 -
bioRxiv
2024 Oct 30:2024.10.30.620736. PMID: 39554043
溶剤 & 溶解度
体外:
DMSO : 9.09 mg/mL (15.71 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (296 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Palea S, et al. Netupitant, a Potent and Highly Selective NK1 Receptor Antagonist, Alleviates Acetic Acid-Induced Bladder Overactivity in Anesthetized Guinea-Pigs. Frontiers in pharmacology. 2016;7:234. [Content Brief]
[2]. Rizzi A, et al. In vitro and in vivo pharmacological characterization of the novel NK₁ receptor selective antagonist Netupitant. Peptides. 2012 Sep;37(1):86-97. [Content Brief]
[3]. Hoffmann T, et al. Design and synthesis of a novel, achiral class of highly potent and selective, orally active neurokinin-1 receptor antagonists. Bioorganic & medicinal chemistry letters. 2006 Mar 01;16(5):1362-5. [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 | 1.7283 mL | 8.6417 mL | 17.2834 mL | 43.2085 mL |
| 5 mM | 0.3457 mL | 1.7283 mL | 3.4567 mL | 8.6417 mL | |
| 10 mM | 0.1728 mL | 0.8642 mL | 1.7283 mL | 4.3208 mL | |
| 15 mM | 0.1152 mL | 0.5761 mL | 1.1522 mL | 2.8806 mL |
Netupitant 関連分類
HY-16346 関連分類
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