Fezolinetant
Based on 5 publication(s) in Google Scholar
Fezolinetant is an antagonist of the neurokinin 3 receptor (NK3R), used for the treatment of menopausal hot flushes.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.19%
- No. CAS: 1629229-37-3
- Fòrmula: C16H15FN6OS
- Peso molecular:358.39
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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
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Fezolinetant
More
Customer Validation & Images
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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In Vivo Efficacy Study
Actividad biológica
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NK3R |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1629229-37-3
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Appearance Solid
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Peso molecular 358.39
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Fòrmula C16H15FN6OS
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Color White to yellow
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SMILES
O=C(N1[C@H](C)C2=NN=C(C3=NC(C)=NS3)N2CC1)C4=CC=C(F)C=C4
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Synonyms
ESN-364
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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 (5)
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Journal Impact Factor
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Most Recent
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Neuron
2026 Jan 8:S0896-6273(25)00927-4. PMID: 41512855
Fezolinetant purchased from MedChemExpress. Usage Cited in: Neuron. 2026 Jan 8:S0896-6273(25)00927-4. [Abstract]
Gastrointestinal transit time (GITT) in adult males (n = 10/group) and females mice (n = 18/group) following administration of Fezolinetant (10 mg/kg; i.p.; single dose) or vehicle.
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J Allergy Clin Immunol
2019 Oct;144(4):1130-1133.e8. PMID: 31405606
Fezolinetant purchased from MedChemExpress. Usage Cited in: J Allergy Clin Immunol. 2019 Oct;144(4):1130-1133.e8. [Abstract]
NK3R antagonist Fezolinetant (10 mg/kg; p.o.; single dose) also selectively inhibits IL-31–induced itch response. Effect of Fezolinetant on scratching behaviors of WT mice in response to various pruritogens. Forty-five minutes before assays, mice (n = 5) were treated with or without Fezolinetant.
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Brain Res
2025 Aug 13:149879. PMID: 40816714
Fezolinetant purchased from MedChemExpress. Usage Cited in: Brain Res. 2025 Aug 13:149879. [Abstract]
Effect of Fezolinetant (1, 5, and 10 mg/kg; i.p.; single dose) administered 30 min after fear acquisition in male mice subjected to the cued-fear conditioning protocol. Fear extinction sessions 1–4, respectively.
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Fezolinetant purchased from MedChemExpress. Usage Cited in: Patent. US20210401821A1.
Fezolinetant (10 mg/kg; p.o.; single dose) reduced the frequency of IL-31-induced scratching behavior but failed to diminish scratching behavior triggered by histamine and chloroquine in wild-type C57BL/6 mice.
Solvente y solubilidad
DMSO : 20 mg/mL (55.81 mM; Need ultrasonic; 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)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2 mg/mL (5.58 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 1% DMSO 99% Saline
Solubility: ≥ 0.2 mg/mL (0.56 mM); Clear solution
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
On the day of the experiment, the NK3R antagonist ESN364 is formulated in physiological saline with 9% 2-hydroxypropyl-β-cyclodextrin at a concentration of 2 mg/mL. At 240 minutes after the initiation of blood sampling, ESN364 (1 mg/kg, n=5) or vehicle (n=5) is administered by an iv bolus injection at a dose volume of 0.5 mL/kg through the jugular cannulae, and the injected material is flushed into the animal with 5 mL of heparinized saline. Blood sampling resumes at the indicated intervals following this iv administration.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (275 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 |
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| DMSO | 1 mM | 2.7903 mL | 13.9513 mL | 27.9026 mL | 69.7564 mL |
| 5 mM | 0.5581 mL | 2.7903 mL | 5.5805 mL | 13.9513 mL | |
| 10 mM | 0.2790 mL | 1.3951 mL | 2.7903 mL | 6.9756 mL | |
| 15 mM | 0.1860 mL | 0.9301 mL | 1.8602 mL | 4.6504 mL | |
| 20 mM | 0.1395 mL | 0.6976 mL | 1.3951 mL | 3.4878 mL | |
| 25 mM | 0.1116 mL | 0.5581 mL | 1.1161 mL | 2.7903 mL | |
| 30 mM | 0.0930 mL | 0.4650 mL | 0.9301 mL | 2.3252 mL | |
| 40 mM | 0.0698 mL | 0.3488 mL | 0.6976 mL | 1.7439 mL | |
| 50 mM | 0.0558 mL | 0.2790 mL | 0.5581 mL | 1.3951 mL |
Fezolinetant Related Classifications
HY-19632 Related Classifications
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