A selective androgen receptor modulator
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GLPG0492

Item No. 29938

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[(4S)-4-(hydroxymethyl)-3-methyl-2,5-dioxo-4-phenyl-1-imidazolidinyl]-2-(trifluoromethyl)-benzonitrile
CAS Number
1215085-92-9
Molecular Formula
C19H14F3N3O3
Formula Weight
389.3
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: slightly solubleEthanol: slightly soluble
SMILES
O=C([C@@](CO)(C1=CC=CC=C1)N2C)N(C3=CC(C(F)(F)F)=C(C#N)C=C3)C2=O
InChi Code
InChI=1S/C19H14F3N3O3/c1-24-17(28)25(14-8-7-12(10-23)15(9-14)19(20,21)22)16(27)18(24,11-26)13-5-3-2-4-6-13/h2-9,26H,11H2,1H3/t18-/m1/s1
InChi Key
VAJGULUVTFDTAS-GOSISDBHSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $423

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    Product 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

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Nique, F., Hebbe, S., Triballeau, N., et al. Identification of a 4-(hydroxymethyl)diarylhydantoin as a selective androgen receptor modulator. J. Med. Chem. 55(19), 8236-8247 (2012).

    2. Cozzoli, A., Capogrosso, R.F., Sblendorio, V.T., et al. GLPG0492, a novel selective androgen receptor modulator, improves muscle performance in the exercised-mdx mouse model of muscular dystrophy. Pharmacol. Res. 72, 9-24 (2013).

    3. Blanqué, R., Lepescheux, L., Auberval, M., et al. Characterization of GLPG0492, a selective androgen receptor modulator, in a mouse model of hindlimb immobilization. BMC Musculoskelet. Disord. 15:291, (2014).