Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
説明 | 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. |
In vitro | 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]. |
分子量 | 389.33 |
分子式 | C19H14F3N3O3 |
CAS No. | 1215085-92-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 45mg/mL (115.6mM)
You can also refer to dose conversion for different animals. 詳細
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GLPG0492 1215085-92-9 Endocrinology/Hormones Androgen Receptor GLPG-0492 GLPG 0492 Inhibitor inhibitor inhibit