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GLPG0492

Catalog No. T11410L CAS 1215085-92-9

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.

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GLPG0492, CAS 1215085-92-9

Pack Size	Availability	Price/USD
1 mg	In stock	$ 139.00
2 mg	In stock	$ 197.00
5 mg	In stock	$ 347.00
10 mg	In stock	$ 497.00
25 mg	In stock	$ 793.00
50 mg	In stock	$ 1,130.00
100 mg	In stock	$ 1,520.00
1 mL * 10 mM (in DMSO)	In stock	$ 382.00

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Purity: 98.27%

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Description

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].

Molecular Weight	389.33
Formula	C19H14F3N3O3
CAS No.	1215085-92-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 45mg/mL (115.6mM)

References and Literature

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.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library ReFRAME Related Library Clinical Compound Library Bioactive Compounds Library Max Bioactive Compound Library Nuclear Receptor Compound Library

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Keywords

GLPG0492 1215085-92-9 Endocrinology/Hormones Androgen Receptor GLPG-0492 GLPG 0492 inhibitor inhibit

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