SR9186
Based on 1 Customer Validation
SR9186 (ML368) is a selective CYP3A4 inhibitor with IC50 values of 9, 4, and 38 nM for Midazolam → 1'-hydroxymidazolam, Testosterone → 6β-hydroxytestosterone, and Vincristine → Vincristine M1, respectively. SR-9186 inhibits the development of hepatic-stage P. falciparum and blocks ivermectin metabolism. SR-9186 can be used in breast cancer research.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.06%
- No. CAS: 1361414-26-7
- Fòrmula: C26H18N6O
- Peso molecular:430.46
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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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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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
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Plasmodium |
CYP3 |
SR-9186 (4 nM-60 μM) selectively inhibits CYP3A4 with IC50 values of 9, 4, and 38 nM for Midazolam, Testosterone, and Vincristine (HY-N0488A) metabolism, respectively[1].
SR-9186 has a long half-life (106 min) in 1 mg/mL human liver microsomes, providing sustained CYP3A4 inhibition[1].
SR-9186 (2.5 μM; 20 min) reduces the formation of Lapatinib (HY-50898)-derived GSH adducts by 78% in pooled human liver microsomes[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1361414-26-7
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Appearance Solid
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Peso molecular 430.46
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Fòrmula C26H18N6O
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Color Yellow to brown
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SMILES
O=C(NC1=CC=C(C2=C3C(NC=N3)=NC=C2)C=C1)NC4=CC=C(C5=CC=C(C#N)C=C5)C=C4
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Synonyms
ML368
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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 : 31.25 mg/mL (72.60 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, 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)
Pureza y Documentación
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Ficha de datos (274 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
[1]. Xiaohai Li, et al. Discovery of a highly selective CYP3A4 inhibitor suitable for reaction phenotyping studies and differentiation of CYP3A4 and CYP3A5. Drug Metab Dispos. 2012 Sep;40(9):1803-9. [Content Brief]
[2]. Towles JK, et al. Cytochrome P450 3A4 and CYP3A5-Catalyzed Bioactivation of Lapatinib. Drug Metab Dispos. 2016 Oct;44(10):1584-97. [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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3231 mL | 11.6155 mL | 23.2310 mL | 58.0774 mL |
| 5 mM | 0.4646 mL | 2.3231 mL | 4.6462 mL | 11.6155 mL | |
| 10 mM | 0.2323 mL | 1.1615 mL | 2.3231 mL | 5.8077 mL | |
| 15 mM | 0.1549 mL | 0.7744 mL | 1.5487 mL | 3.8718 mL | |
| 20 mM | 0.1162 mL | 0.5808 mL | 1.1615 mL | 2.9039 mL | |
| 25 mM | 0.0929 mL | 0.4646 mL | 0.9292 mL | 2.3231 mL | |
| 30 mM | 0.0774 mL | 0.3872 mL | 0.7744 mL | 1.9359 mL | |
| 40 mM | 0.0581 mL | 0.2904 mL | 0.5808 mL | 1.4519 mL | |
| 50 mM | 0.0465 mL | 0.2323 mL | 0.4646 mL | 1.1615 mL | |
| 60 mM | 0.0387 mL | 0.1936 mL | 0.3872 mL | 0.9680 mL |
SR9186 Related Classifications
HY-120696 Related Classifications
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