Product Code：S007083
English Name：Sitagliptin Impurity 83
English Alias：7-nitroso-3-(trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine
CAS No.：2892260-32-9
Molecular Formula：C₆H₆F₃N₅O
Molecular Weight：221.14
High-Purity Reference Standard：Confirmed by HPLC (≥99.0%), NMR (1H, 13C), HRMS, and elemental analysis, suitable for Sitagliptin impurity analysis and quality control.
Stability Assurance：Stable for 36 months at -20℃ under light-protected, sealed storage; degradation rate <0.2% in acetonitrile-water solution within 6 months.
Quality Control Testing：Used for UPLC-MS/MS detection of Impurity 83 in Sitagliptin API and formulations, controlling content to meet ICH Q3A standards (single impurity limit ≤0.1%).
Process Optimization Research：Monitors Impurity 83 formation during Sitagliptin synthesis, reducing generation by >50% by adjusting cyclization temperature (e.g., 60-70℃) and reaction time.
Method Validation：Serves as a standard for developing impurity detection methods, verifying UPLC resolution (≥3.0) and LOD (0.005 ng/mL).
Sitagliptin, a dipeptidyl peptidase-4 (DPP-4) inhibitor, is used for treating type 2 diabetes. Impurity 83, as a process-related impurity of Sitagliptin, may originate from incomplete intermediate reactions or side reactions during multi-step synthesis. Its trifluoromethyl and nitroso groups may affect drug stability and safety. With stricter FDA and EMA requirements for diabetes drug impurities, studying Impurity 83 is crucial for ensuring drug quality.
Detection Technology：UPLC-MS/MS with C18 column (1.7μm) and 0.1% formic acid-acetonitrile gradient elution achieves separation within 3 minutes, with LOD of 0.002 ng/mL for trace impurity analysis.
Formation Mechanism：Mainly formed during the nitrosation of triazolopyrazine rings. Optimizing the reaction solvent system (e.g., using DMF instead of methanol) and controlling nitrosating agent dosage inhibits its formation.
Safety Evaluation：In vitro cytotoxicity shows IC₅₀ of 168.3 μM against HepG2 cells (Sitagliptin IC₅₀=12.5 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.
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!
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