LGD-3303

Recently, the selective androgen receptor modulators (SARMs) have been popular among athletes due to their muscle strengthening effects.However, it has been often reported that the unauthorized compounds like SARMs were illegally adulterated in dietary supplements and were misused to improve their pharmacol. efficacies.To analyze and reconfirm the SARMs adulterated in dietary supplements, we developed and optimized a rapid and accurate method to measure 18 SARMs simultaneously using an ultra-high-performance liquid chromatog. system equipped with a photodiode array detector and liquid chromatog.-electrospray ionization-tandem mass spectrometry.The simultaneous methods were validated to fully meet the international guidelines by determining the limit of detection, limit of quantification, method detection limit, method quantitation limit, specificity, linearity, precision, accuracy, recovery, stability, and matrix effect.In addition, the validated methods were used for application to 75 real samples containing dietary supplements and seized samples.On screening 18 compounds, a total 10 SARMs (MK-677, YK-11, etc.) were detected in 25 seized hard capsule samples by comparing the UHPLC-PDA and LC-ESI-MS/MS.In addition, the concentrations of adulterants in seized hard capsule samples ranged from min. at 2.14μg g-1 of LGD-4033 and maximum at 71,989μg g-1 of andarine.The established simultaneous anal. method could help to investigate the unauthorized compounds adulterated in various types of dietary supplement.

Selective androgen receptor modulators, SARMs, are a large class of compounds developed to provide therapeutic anabolic effects with minimal androgenic side effects. A wide range of these compounds are available to purchase online and thus provide the potential for abuse in sports. Knowledge of the metabolism of these compounds is essential to aid their detection in doping control samples. In vitro models allow a quick, cost‐effective response where administration studies are yet to be carried out. In this study, the equine phase I metabolism of the non‐steroidal SARMs GSK2881078, LGD‐2226, LGD‐3303, PF‐06260414, ACP‐105, RAD‐140 and S‐23 was investigated using equine liver microsomes. Liquid chromatography coupled to a QExactive Orbitrap mass spectrometer allowed identification of metabolites with high resolution and mass accuracy. Three metabolites were identified for both GSK2881078 and LGD‐2226, four for LGD‐3303 and RAD‐140, five for PF‐06260414, twelve for ACP‐105 and ten for S‐23. The equine metabolism of GSK‐2881078, LGD‐2226, LGD‐3303 and PF‐06260414 is reported for the first time. Although the equine metabolism of ACP‐105, RAD‐140 and S‐23 has previously been reported, the results obtained in this study have been compared with published data.