GLPG0492

Modify Date: 2024-01-14 06:25:49

GLPG0492 Structure
GLPG0492 structure
Common Name GLPG0492
CAS Number 1215085-92-9 Molecular Weight 389.328
Density 1.5±0.1 g/cm3 Boiling Point 544.0±60.0 °C at 760 mmHg
Molecular Formula C19H14F3N3O3 Melting Point N/A
MSDS N/A Flash Point 282.8±32.9 °C

 Use of GLPG0492


GLPG0492 is a novel selective androgen receptor modulator; exhibited anabolic activity on muscle, strongly dissociated from the androgenic activity on prostate after oral dosing.IC50 value:Target: AR modulatorGLPG0492 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 androgen receptor modulator that is currently under development for musculo-skeletal diseases such as sarcopenia and 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 a significant increase in fatigue (30-50%) [2]. GLPG0492 treatment partially prevents immobilization-induced muscle atrophy with a trend to promote muscle fiber hypertrophy in a dose-dependent manner. Interestingly, GLPG0492 was found as efficacious as TP at reducing muscle loss while sparing reproductive tissues. 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].

 Names

Name GLPG0492
Synonym More Synonyms

 GLPG0492 Biological Activity

Description GLPG0492 is a novel selective androgen receptor modulator; exhibited anabolic activity on muscle, strongly dissociated from the androgenic activity on prostate after oral dosing.IC50 value:Target: AR modulatorGLPG0492 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 androgen receptor modulator that is currently under development for musculo-skeletal diseases such as sarcopenia and 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 a significant increase in fatigue (30-50%) [2]. GLPG0492 treatment partially prevents immobilization-induced muscle atrophy with a trend to promote muscle fiber hypertrophy in a dose-dependent manner. Interestingly, GLPG0492 was found as efficacious as TP at reducing muscle loss while sparing reproductive tissues. 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].
Related Catalog
References

[1]. Nique F, et al. Identification of a 4-(hydroxymethyl)diarylhydantoin as a selective androgen receptor modulator. 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 mouse model of hindlimb immobilization. BMC Musculoskelet Disord. 2014 Sep 3;15:291.

 Chemical & Physical Properties

Density 1.5±0.1 g/cm3
Boiling Point 544.0±60.0 °C at 760 mmHg
Molecular Formula C19H14F3N3O3
Molecular Weight 389.328
Flash Point 282.8±32.9 °C
Exact Mass 389.098724
LogP 2.07
Vapour Pressure 0.0±1.5 mmHg at 25°C
Index of Refraction 1.627
Storage condition 2-8℃

 Synonyms

GLPG-0492
Benzonitrile, 4-[(4S)-4-(hydroxymethyl)-3-methyl-2,5-dioxo-4-phenyl-1-imidazolidinyl]-2-(trifluoromethyl)-
4-[(4S)-4-(Hydroxymethyl)-3-methyl-2,5-dioxo-4-phenyl-1-imidazolidinyl]-2-(trifluoromethyl)benzonitrile
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  • DC Chemicals Limited
  • China
  • Product Name: GLPG-0492
  • Price: $Inquiry/100mg $Inquiry/250mg $Inquiry/1g
  • Purity: 98.0%
  • Stocking Period: 3 Day
  • Contact: Tony Cao


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Price: $462/10mM*1mLinDMSO

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