| Identification | Back Directory | [Name]
GLPG 0492 | [CAS]
1215085-92-9 | [Synonyms]
GLPG 0492
GLPG-0492
(GLPG0492)
4-[(4S)-4-(Hydroxymethyl)-3-methyl-2,5-dioxo-4-phenyl-1-imidazolidinyl]-2-(trifluoromethyl)benzonitrile
Benzonitrile, 4-[(4S)-4-(hydroxymethyl)-3-methyl-2,5-dioxo-4-phenyl-1-imidazolidinyl]-2-(trifluoromethyl)- | [Molecular Formula]
C19H14F3N3O3 | [MOL File]
1215085-92-9.mol | [Molecular Weight]
389.33 |
| Chemical Properties | Back Directory | [Melting point ]
66 - 71°C | [Boiling point ]
544.0±60.0 °C(Predicted) | [density ]
1.50±0.1 g/cm3(Predicted) | [storage temp. ]
Hygroscopic, -20°C Freezer, Under inert atmosphere | [solubility ]
DMSO (Slightly), Ethanol (Slightly, Sonicated) | [form ]
Solid | [pka]
13.50±0.10(Predicted) | [color ]
White to Off-White | [Stability:]
Hygroscopic |
| Hazard Information | Back Directory | [Description]
GLPG0492 is a selective androgen receptor modulator (SARM).1 It activates the androgen receptor in a transactivation assay (EC50 = 12 nM in HeLa cells expressing the human receptor). GLPG0492 (10 mg/kg per day) increases levator ani muscle weight, a marker of anabolic activity, but has no effect on ventral prostate weight, a marker of androgenic activity, in castrated rats. It increases twitch tension in isolated diaphragm strips, as well as increases the total distance run in a treadmill test and decreases gastrocnemius muscle fibrosis in the exercised-mdx mouse model of muscular dystrophy when administered at a dose of 30 mg/kg.2 GLPG0492 also reverses immobilization-induced muscle atrophy in a mouse model of hindlimb immobilization.3 | [Uses]
GLPG-0492 is a non-steroidal Selective Androgen Receptor Modulator (SARM), which can be used to reduce muscle loss while sparing reproductive tissues. | [References]
[1] FRAN?OIS NIQUE. Identification of a 4-(Hydroxymethyl)diarylhydantoin as a Selective Androgen Receptor Modulator[J]. Journal of Medicinal Chemistry, 2012, 55 19: 8236-8247. DOI: 10.1021/jm300281x
[2] ANNA COZZOLI . GLPG0492, a novel selective androgen receptor modulator, improves muscle performance in the exercised-mdx mouse model of muscular dystrophy[J]. Pharmacological research, 2013, 72: Pages 9-24. DOI: 10.1016/j.phrs.2013.03.003
[3] ROLAND BLANQUé. Characterization of GLPG0492, a selective androgen receptor modulator, in a mouse model of hindlimb immobilization.[J]. BMC Musculoskeletal Disorders, 2014, 15: 291. DOI: 10.1186/1471-2474-15-291 |
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