Product Name:CAS No.: Cat. No.:MWt:Formula:Purity :
GLPG04921215085-92-9HY-18102389.33
C19H14F3N3O3>98%
Solubility:DMSO
Mechanisms:
Pathways:Others; Target:Androgen Receptor
Biological Activity:
GLPG0492 is a novel selective androgen receptor modulator; exhibited anabolic activity on muscle, stronglydissociated from the androgenic activity on prostate after oral dosing. IC50 value:
Target: 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]. GLPG0492 is a new non-steroidal selective androgenreceptor modulator that is currently under development for musculo-skeletal diseases such as sarcopeniaand cachexia. In acute exhaustion tests, a surrogate of the 6-min walking test used in DMD patients,GLPG0492 preserved running performance, whereas vehicle- or comparator-treated animals showed asignificant increase in fatigue (30-50%) [2]. GLPG0492 treatment partially prevents immobilization-inducedmuscle atrophy with a trend to promote muscle fi...References:
[1]. Nique F, et al. Identification of a 4-(hydroxymethyl)diarylhydantoin as a selective androgen receptormodulator. J Med Chem. 2012 Oct 11;55(19):8236-47.
[2]. Cozzoli A, et al. GLPG0492, a novel selective androgen receptor modulator, improves muscle
performance in the exercised-mdx mouse model of muscular dystrophy. Pharmacol Res. 2013 Jun;72:9-24. [3]. Blanqué R, et al. Characterization of GLPG0492, a selective androgen receptor modulator, in a mousemodel of hindlimb immobilization. BMC Musculoskelet Disord. 2014 Sep 3;15:291.
Caution: Not fully tested. For research purposes only
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