Elinzanetant
Based on 1 Customer Validation
Elinzanetant is an orally active and selective NK-1 and NK-3 receptor antagonist. Elinzanetant alleviates menopause-associated vasomotor symptoms, including hot flashes and night sweats. Elinzanetant reduces estradiol and progesterone levels. Elinzanetant can be used for the research of moderate to severe vasomotor and sleep disorders associated with menopause.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.82%
- No. CAS: 929046-33-3
- Fòrmula: C33H35F7N4O3
- Peso molecular:668.64
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
The metabolism of Elinzanetant in human hepatocytes and liver microsomes is mainly mediated by CYP3A4 (81% of CYP3A contribution), with a small amount of glucuronidation occurring simultaneously[1].
Elinzanetant (10 μM; 24 h) remains stable in fresh human feces under anaerobic conditions at 37℃[1].
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 929046-33-3
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Appearance Solid
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Peso molecular 668.64
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Fòrmula C33H35F7N4O3
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Color White to light yellow
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SMILES
CC(C)(C1=CC(C(F)(F)F)=CC(C(F)(F)F)=C1)C(N(C2=CN=C(N3[C@@H](CN4[C@@](COCC4)([H])C3)CO)C=C2C5=C(C=C(C=C5)F)C)C)=O
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Synonyms
NT-814; BAY3427080
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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 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (149.56 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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: ≥ 2.5 mg/mL (3.74 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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.
Pureza y Documentación
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Ficha de datos (277 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Schulz SI, et al. Mass Balance Recovery, Absorption, Metabolism, and Excretion of Elinzanetant in Healthy Human Volunteers and in vitro Biotransformation. Eur J Drug Metab Pharmacokinet. 2025;50(1):91-103. [Content Brief]
[2]. Pawsey S, et al. Elinzanetant (NT-814), a Neurokinin 1,3 Receptor Antagonist, Reduces Estradiol and Progesterone in Healthy Women. J Clin Endocrinol Metab. 2021 Jul 13;106(8):e3221-e3234. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.4956 mL | 7.4779 mL | 14.9557 mL | 37.3893 mL |
| 5 mM | 0.2991 mL | 1.4956 mL | 2.9911 mL | 7.4779 mL | |
| 10 mM | 0.1496 mL | 0.7478 mL | 1.4956 mL | 3.7389 mL | |
| 15 mM | 0.0997 mL | 0.4985 mL | 0.9970 mL | 2.4926 mL | |
| 20 mM | 0.0748 mL | 0.3739 mL | 0.7478 mL | 1.8695 mL | |
| 25 mM | 0.0598 mL | 0.2991 mL | 0.5982 mL | 1.4956 mL | |
| 30 mM | 0.0499 mL | 0.2493 mL | 0.4985 mL | 1.2463 mL | |
| 40 mM | 0.0374 mL | 0.1869 mL | 0.3739 mL | 0.9347 mL | |
| 50 mM | 0.0299 mL | 0.1496 mL | 0.2991 mL | 0.7478 mL | |
| 60 mM | 0.0249 mL | 0.1246 mL | 0.2493 mL | 0.6232 mL | |
| 80 mM | 0.0187 mL | 0.0935 mL | 0.1869 mL | 0.4674 mL | |
| 100 mM | 0.0150 mL | 0.0748 mL | 0.1496 mL | 0.3739 mL |
Elinzanetant Related Classifications
HY-109171 Related Classifications
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- Elinzanetant
- 929046-33-3
- NT-814
- BAY3427080
- NT814
- NT 814
- BAY3427080
- BAY 3427080
- BAY-3427080
- Neurokinin Receptor
- sex-steroid-deficient states
- human hepatocytes
- CYP3A4
- neurokinin-1 receptor
- menopausal vasomotor symptoms
- night sweats
- neurokinin B
- neurokinin-3 receptor
- hot flushes
- liver microsomes
- Inhibitor
- inhibitor
- inhibit