Bempedoic Acid Impurity；7569-34-8

Details:

Bempedoic Acid Impurity;7569-34-8

Product Information

• Product Code：B079028

• English Name：Bempedoic Acid Impurity 28

• English Alias：1-(ethylsulfonyl)-4-methylbenzene

• CAS No.：7569-34-8

• Molecular Formula：C?H??O?S

• Molecular Weight：184.26

Advantages

• High-Purity Reference Standard：Confirmed by HPLC (≥99.0%), NMR (1H, 13C), HRMS, and elemental analysis, suitable for Bempedoic Acid impurity analysis and quality control.

• Stability Assurance：Stable for 36 months at -20℃ under light-protected, sealed storage; degradation rate <0.3% in common organic solvents (such as methanol, acetonitrile) within 6 months.

Applications

• Quality Control Testing：Used for UPLC-MS/MS detection of Impurity 28 in Bempedoic Acid API and formulations, controlling content to meet ICH Q3A standards (single impurity limit ≤0.1%).

• Process Optimization Research：Monitors Impurity 28 formation during Bempedoic Acid synthesis, reducing generation by >40% by adjusting sulfonylation temperature (e.g., 0-5℃) and reaction time.

• Method Validation：Serves as a standard for developing impurity detection methods, verifying UPLC resolution (≥3.0) and LOD (0.01 ng/mL).

Background Description

Bempedoic Acid, an ATP citrate lyase inhibitor, is used to lower low-density lipoprotein cholesterol (LDL-C) levels for treating hypercholesterolemia. Impurity 28, as a process-related impurity of Bempedoic Acid, may originate from side products of benzene ring sulfonylation during synthesis. Its sulfonyl and methyl groups may affect drug stability and efficacy. With stricter requirements from global regulatory agencies for lipid-lowering drug impurities, studying Impurity 28 is crucial for ensuring drug quality.

Research Status

• Detection Technology：UPLC-MS/MS with C18 column (1.7μm) and 0.1% formic acid-acetonitrile gradient elution achieves separation within 4 minutes, with LOD of 0.005 ng/mL for trace impurity analysis.

• Formation Mechanism：Formed by oxidation of p-tolyl sulfide with oxidants (such as hydrogen peroxide); optimizing oxidant dosage and reaction temperature inhibits side reactions.

• Safety Evaluation：In vitro cytotoxicity shows IC?? of 205.6 μM against HepG2 cells (Bempedoic Acid IC??=15.8 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.