N-Desmethyl-Apalutamide
Based on 1 publication(s) in Google Scholar
N-Desmethyl-Apalutamide, the major active metabolite of Apalutamide (HY-16060), is a selective competitive inhibitor of androgen receptor. N-Desmethyl-Apalutamide is catalyzed by CYP3A4 and CYP2C8 enzymes. The plasma protein binding rate of N-Desmethyl-Apalutamide reaches 95%, with albumin as the primary binding protein. N-Desmethyl-Apalutamide is suitable for prostate cancer-related research.
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- Pureza : 99.08%
- No. CAS: 1332391-11-3
- Fòrmula: C20H13F4N5O2S
- Peso molecular:463.41
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) N-Desmethyl-Apalutamide
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Actividad biológica
Descripciòn
IC50 & Target
[2]|
CYP2C8 |
CYP3A4 |
In Vitro
N-Desmethyl-Apalutamide, the primary bioactive metabolite of Apalutamide (HY-1606), tightly binds androgen receptor and shows a plasma protein binding fraction of 95%[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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No. CAS 1332391-11-3
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Appearance Solid
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Peso molecular 463.41
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Fòrmula C20H13F4N5O2S
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Color White to off-white
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SMILES
O=C(N)C1=CC=C(N(C(N(C2=CC(C(F)(F)F)=C(C#N)N=C2)C3=O)=S)C43CCC4)C=C1F
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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
Publications (1)
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Journal Impact Factor
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Most Recent
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J Pharm Health Care Sci
Simultaneous measurement of apalutamide and N-desmethylapalutamide in human plasma using high-performance liquid chromatography with ultraviolet detection. [Abstract]2025 Sep 29;11(1):84. PMID: 41024304
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (215.79 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)
Protocolo
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Immunoprecipitation
Immunoprecipitation (IP) is an experimental method that uses the principle of antibody specific binding to purify and enrich target proteins.
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Research Protocol for Endocrine Diseases
Endocrine diseases often arise from disrupted hormone production, hormone signaling, or target-tissue responsiveness; for diabetes-focused endocrine disease models, insulin signaling regulates glucose uptake, hepatic glucose output, lipid metabolism, and β-cell compensation. Type 2 diabetes develops through interacting defects in insulin resistance, β-cell dysfunction, adipose inflammation, hepatic glucose overproduction, altered incretin signaling, and ectopic lipid metabolism. A major unresolved question is whether endocrine dysfunction is driven primarily by target-tissue insulin resistance, intrinsic β-cell failure, immune/inflammatory stress, or combined multi-organ failure that differs by disease stage.
Pureza y Documentación
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Ficha de datos (279 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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, 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1579 mL | 10.7896 mL | 21.5792 mL | 53.9479 mL |
| 5 mM | 0.4316 mL | 2.1579 mL | 4.3158 mL | 10.7896 mL | |
| 10 mM | 0.2158 mL | 1.0790 mL | 2.1579 mL | 5.3948 mL | |
| 15 mM | 0.1439 mL | 0.7193 mL | 1.4386 mL | 3.5965 mL | |
| 20 mM | 0.1079 mL | 0.5395 mL | 1.0790 mL | 2.6974 mL | |
| 25 mM | 0.0863 mL | 0.4316 mL | 0.8632 mL | 2.1579 mL | |
| 30 mM | 0.0719 mL | 0.3597 mL | 0.7193 mL | 1.7983 mL | |
| 40 mM | 0.0539 mL | 0.2697 mL | 0.5395 mL | 1.3487 mL | |
| 50 mM | 0.0432 mL | 0.2158 mL | 0.4316 mL | 1.0790 mL | |
| 60 mM | 0.0360 mL | 0.1798 mL | 0.3597 mL | 0.8991 mL | |
| 80 mM | 0.0270 mL | 0.1349 mL | 0.2697 mL | 0.6743 mL | |
| 100 mM | 0.0216 mL | 0.1079 mL | 0.2158 mL | 0.5395 mL |