A selective androgen receptor modulator; activates the androgen receptor in a transactivation assay (EC50 = 12 nM in HeLa cells expressing the human receptor); increases levator ani muscle weight

GLPG0492 – 1 mg

Brand:
Cayman
CAS:
1215085-92-9
Storage:
-20
UN-No:
Non-Hazardous - /

GLPG0492 is a selective androgen receptor modulator (SARM).{53473} 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.{53474} GLPG0492 also reverses immobilization-induced muscle atrophy in a mouse model of hindlimb immobilization.{53475}  

 

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Description

A selective androgen receptor modulator; activates the androgen receptor in a transactivation assay (EC50 = 12 nM in HeLa cells expressing the human receptor); increases levator ani muscle weight, but has no effect on prostate weight, in castrated rats at 10 mg/kg per day; 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 at 30 mg/kg; reverses immobilization-induced muscle atrophy in a mouse model of hindlimb immobilization

Formal name: 4-[(4S)-4-(hydroxymethyl)-3-methyl-2,5-dioxo-4-phenyl-1-imidazolidinyl]-2-(trifluoromethyl)-benzonitrile

Synonyms: 

Molecular weight: 389.3

CAS: 1215085-92-9

Purity: ≥98%

Formulation: A solid

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