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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.90%
- No. CAS: 290297-26-6
- Fòrmula: C30H32F6N4O
- Peso molecular:578.59
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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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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- Referencias
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Publications Citing Use of MedChemExpress (MCE) Netupitant
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Actividad biológica
Descripciòn
IC50 & Target
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hNK1 |
In Vitro
Netupitant potently and selectively inhibits NK1 receptor-mediated contractions in isolated guinea pig detrusor muscle strips, with a mean pKB value of 9.24[1].
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. .
In Vivo
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.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 290297-26-6
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Appearance Solid
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Peso molecular 578.59
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Fòrmula 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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Synonyms
CID 6451149
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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 (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
Solvente y solubilidad
In Vitro:
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (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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Instrucciones de manejo (2659 KB)
Referencias
[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 Related Classifications
HY-16346 Related Classifications
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