LY2452473 is a selective androgen receptor modulator (SARM)[1-2]. LY2452473 can be used in research related to prostate cancer and hypogonadism-associated conditions[3-4].
In vitro, PC12 cells were treated with LY2452473 (0.1nM-10µM) for 12 hours. LY2452473 dose-dependently and highly selectively antagonized AR activity and inhibited the MAPK signaling pathway. Additionally, LY2452473 activated the cAMP signaling pathway[5].
References:
[1] Mazzarino M, Di Costanzo L, Comunità F, et al. UHPLC-HRMS Method for the Simultaneous Screening of 235 Drugs in Capillary Blood for Doping Control Purpose: Comparative Evaluation of Volumetric and Non-volumetric Dried Blood Spotting Devices. ACS Omega. 2022 Aug 29;7(36):31845-31868
[2] Stacchini C, Botrè F, Comunità F, et al. Simultaneous detection of different chemical classes of selective androgen receptor modulators in urine by liquid chromatography-mass spectrometry-based techniques. J Pharm Biomed Anal. 2021 Feb 20;195:113849.
[3] Piper T, Heimbach S, Adamczewski M, et al. An in vitro assay approach to investigate the potential impact of different doping agents on the steroid profile. Drug Test Anal. 2021 May;13(5):916-928.
[4] Karatt TK, Sathiq MA, Laya S, et al. Metabolic study of selective androgen receptor modulator LY2452473 in thoroughbred horses for doping control. Rapid Commun Mass Spectrom. 2023 May 15;37(9):e9491.
[5] Popović L, Brankatschk B, Palladino G, et al. Polypharmacological profiling across protein target families and cellular pathways using the multiplexed cell-based assay platform safetyProfiler reveals efficacy, potency and side effects of drugs. Biomed Pharmacother. 2024 Nov;180:117523.
LY2452473是一种选择性雄激素受体（AR）调节剂（SARM） [1-2]。LY2452473可用于前列腺癌和与性腺功能减退相关疾病的研究[3-4]。
在体外，LY2452473（0.1nM-10μM）处理PC12细胞12小时。LY2452473可剂量依赖性地、高选择性地拮抗Ar的活性和抑制MAPK信号通路，LY2452473可激活cAMP信号通路[5]。