GLPG0492 是一种非甾体选择性雄激素受体 (Androgen Receptor) 调节剂。GLPG0492 在肌肉骨骼疾病如肌萎缩和恶病质的研究方面具有潜在的潜力。

GLPG0492 is a novel selective androgen receptor modulator. After oral dosing, it showed anabolic activity on muscle, strongly dissociated from the androgenic activity on the prostate.

GLPG0492 is a new non-steroidal selective androgen receptor modulator that is currently under development for musculo-skeletal diseases such as sarcopenia and cachexia. GLPG0492 was found as efficacious as TP at reducing muscle loss while sparing reproductive tissues. GLPG0492 treatment partially prevents immobilization-induced muscle atrophy with a trend to promote muscle fiber hypertrophy in a dose-dependent manner. AR modulator GLPG0492 has very good pharmacokinetic properties, including bioavailability in rat (F >50%), and is currently under evaluation in phase I clinical trials [1]. A surrogate of the 6-min walking test used in DMD patients, GLPG0492 preserved running performance, in acute exhaustion tests. Whereas vehicle- or comparator-treated animals showed a significant increase in fatigue (30-50%) [2]. Furthermore, gene expression studies performed on tibialis samples revealed that both GLPG0492 and TP were slowing down muscle loss by negatively interfering with major signaling pathways controlling muscle mass homeostasis [3].

1215085-92-9

C19H14F3N3O3

389.33

DMSO:45mg/mL (115.6mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years