(-)-PX20606 trans isomer ((-)-PX-102 trans isomer) 是一种 FXR 激动剂,在 FRET 和 M1H 试验中对 FXR 的 EC50 分别为 18 和 29 nM。
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(-)-PX20606 trans isomer is a FXR agonist with EC50s of 18 and 29 nM for FXR in FRET and M1H assay, respectively.
[1]. Kinzel O, et al. Novel substituted isoxazole FXR agonists with cyclopropyl, hydroxycyclobutyl and hydroxyazetidinyl linkers: Understanding and improving key determinants of pharmacological properties. Bioorg Med Chem Lett. 2016 Aug 1;26(15):3746-53.