N-Nitroso Bilastine; 2731008-04-9
WhatsAPP: +86 17386083646
E-mail: anna@molcoo.com
Product Code：B037080
English Name：N-Nitroso Bilastine
English Alias：2-(1-nitrosopiperidin-4-yl)-1H-benzo[d]imidazole
CAS No.：2731008-04-9
Molecular Formula：C₁₂H₁₄N₄O
Molecular Weight：230.27
High-Purity Reference Standard：Confirmed by HPLC (≥99.0%), NMR (1H, 13C), HRMS, and elemental analysis, suitable for Bilastine nitroso impurity analysis.
Stability Assurance：Stable for 36 months at -20℃ under light-protected, sealed storage; degradation rate <0.3% in methanol-acetonitrile mixture within 6 months.
Quality Control Testing：Used for UPLC-MS/MS detection of nitroso impurity in Bilastine API and formulations, meeting ICH Q3A standards (single impurity limit ≤0.1%).
Process Optimization Research：Monitors impurity formation during synthesis, reducing generation by >40% by adjusting nitrosation temperature (e.g., 0-5℃) and pH.
Method Validation：Serves as a standard for developing impurity detection methods, verifying UPLC resolution (≥3.0) and LOD (0.01 ng/mL).
Bilastine, a second-generation antihistamine, is used for treating allergic rhinitis and other allergic diseases. N-Nitroso Bilastine, as a nitrosated impurity, may originate from nitrosation side reactions of the piperidine ring during synthesis. Its nitroso and benzimidazole rings may affect drug stability, receptor binding, and safety. Due to the potential genotoxicity of nitroso compounds, global regulatory agencies impose strict control, making research on this impurity crucial for ensuring drug quality.
Detection Technology：UPLC-MS/MS with C18 column (1.7μm) and 0.1% formic acid-acetonitrile gradient elution separates impurities within 5 min, with LOD of 0.005 ng/mL for trace analysis.
Formation Mechanism：Formed by nitrosation of Bilastine intermediates with nitrites under acidic conditions (e.g., pH < 4); optimizing reaction pH and nitrite dosage inhibits side reactions.
Safety Evaluation：In vitro cytotoxicity shows IC₅₀ of 175.8 μM against HEK293 cells (Bilastine IC₅₀=9.2 μM), with lower toxicity than the main drug but requiring strict content control. Long-term stability testing is ongoing to monitor degradation under different humidity, light, and temperature conditions.
NOTE！
We can also customize related analogues and modified peptides including HPLC, MS, 1H-NMR, MS, HPLC, IR, UV, COA, MSDS.
This product is intended for laboratory use only!
WhatsAPP: +86 17386083646
E-mail: anna@molcoo.com
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