N-Nitroso Bisoprolol
Product Code：N031049
English Name：N-Nitroso Bisoprolol
English Alias：N-(2-hydroxy-3-(4-((2-isopropoxyethoxy)methyl)phenoxy)propyl)-N-isopropylnitrous amide
CAS No.：2820170-76-9
Molecular Formula：C18H30N2O5
Molecular Weight：354.44
High Purity Guarantee：Confirmed by HPLC (≥99.0%), combined with NMR (1H, 13C), HRMS, and elemental analysis, ensuring the accuracy and reliability of impurity analysis.
Excellent Stability：Stable for 36 months at -20℃ under light-protected, sealed storage; degradation rate <0.2% in acetonitrile - water solution within 6 months, ensuring high reproducibility of experimental data.
Quality Control Testing：Used for UPLC - MS/MS detection of N - nitroso impurities in Bisoprolol API and formulations, strictly controlling impurity content to meet ICH M7 standards (genotoxic impurity limit ≤1.5 μg/day).
Process Optimization Research：Monitor the formation of N - Nitroso Bisoprolol from nitrosation side reactions during Bisoprolol synthesis or storage. Reduce impurity generation by over 60% by adjusting reaction temperature (e.g., 5 - 10℃), avoiding nitrite exposure, or adding antioxidants.
Method Validation：Serves as a standard for developing nitrosamine impurity detection methods, verifying UPLC resolution (≥3.0) and LOD (0.005 ng/mL) to ensure the sensitivity and specificity of the detection method.
Bisoprolol is a β - blocker widely used in the treatment of hypertension, angina pectoris, and chronic heart failure. N - Nitroso Bisoprolol, as a potential genotoxic impurity (GTI), may be formed by the reaction between amine structures and nitrites during Bisoprolol production or through spontaneous nitrosation under acidic and high - temperature storage conditions. Its nitrosamide group poses mutagenic and carcinogenic risks. With increasingly strict regulations on GTIs by global regulatory agencies (such as FDA and EMA), the study of this impurity has become a crucial part of ensuring drug safety and compliance.
Detection Technology：UPLC - MS/MS with a C18 column (1.7μm) and 0.1% formic acid - acetonitrile gradient elution achieves separation within 3 minutes, with an LOD as low as 0.002 ng/mL, enabling highly sensitive detection of trace nitrosamine impurities.
Formation Mechanism：Studies show that this impurity is formed by the reaction of the amino group in Bisoprolol with sodium nitrite under acidic conditions (pH＜4). It can be effectively inhibited by optimizing the reaction system pH to neutral, using inert gas protection, or replacing the synthesis route without nitrosation risk.
Safety Evaluation：In vitro Ames tests confirm the mutagenicity of this impurity, and toxicological studies determine its permitted daily intake (TTC value) as 1.5 μg/day. Currently, accelerated stability tests are being conducted to systematically monitor its nitrosation rate under different humidity, light, and temperature conditions, aiming to improve risk control strategies.
This product is intended for laboratory use only!
WhatsAPP: +86 17320513646
E-mail: anna@molcoo.com
NEW IN STOCK!
The Molcoo Laboratory added drug impurity reference standards, including Baricitinib, Piperazine, Benzylpenicillin, Tranilast and multiple N-Nitroso drug impurities! Now available for immediate delivery!
China
