GLPG0492
CAS No. : 1215085-92-9
Price and Availability of
CAS No. : 1215085-92-9
| Size | Price | Stock |
|---|---|---|
| 5mg | $340 | In-stock |
| 10mg | $500 | In-stock |
| 50mg | $1150 | In-stock |
| 100mg | $1550 | In-stock |
| 200 mg | Get quote | |
| 500 mg | Get quote | |
| We match the lowest price on market. | ||
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| Cat. No. : | HY-18102 |
| M.Wt: | 389.33 |
| Formula: | C19H14F3N3O3 |
| Purity: | >98 % |
| Solubility: | DMSO : ≥ 50 mg/mL |
Introduction of
1215085-92-9
:
GLPG0492 (10−11-10−5 M; 24 h) acts as an androgen agonist in human PC3 (AR) 2 prostate cancer cells, with an EC50 of 1.24 × 10−8 M, and this agonistic activity is antagonized by the antiandrogen drug bicalutamide (HY-14249)[1]. In Vivo:GLPG0492 (30 mg/kg; s.c.; once daily, 6 days per week; for 4 consecutive weeks) significantly improves in vivo forelimb strength and exercise endurance in mdx mice after exercise, enhances diaphragmatic contractile function, reduces diaphragmatic fibrosis, and improves the levels of EDL muscle cell injury markers[2].
GLPG0492 (0.3-30 mg/kg; s.c.; once daily, 6 days per week for 12 weeks) significantly enhances long-term forelimb strength and exercise endurance in mdx mice after exercise, improves the functions of the diaphragm and EDL muscle, reduces the degeneration-regeneration cycle and fibrosis of the diaphragm, and ameliorates cell damage markers in the EDL muscle, with a plateau effect often observed at low doses[2].
GLPG0492 (0.3-30 mg/kg; s.c.; 6 days per week; for 4 to 12 weeks) significantly increases forelimb grip strength, maintains running capacity, improves muscle electrophysiological and histological parameters, and exhibits a dose-dependent therapeutic effect in exercised mdx mice (a model of Duchenne muscular dystrophy)[3].
GLPG0492 (0.3-10 mg/kg; s.c.; once daily for 7 consecutive days) dose-dependently alleviates hindlimb immobilization-induced muscle atrophy in male BALB/cj mice; at doses of 3 and 10 mg/kg/day, it exerts maximal improving effects on muscle mass and myofiber size, without causing damage to reproductive tissues, and regulates key muscle atrophy signaling pathways related to mitochondrial bioenergetics and plasma metabolic markers[4].
GLPG0492 is an orally active, non-steroidal selective androgen receptor modulator. GLPG0492 exerts functional transactivation by binding to the ligand-binding domain of the receptor, exhibiting preferential partial agonist activity in muscle and bone tissues with low activity in reproductive tissues. GLPG0492 effectively counteracts muscle atrophy-related pathways, significantly enhances muscle strength, maintains motor ability, reduces fibrosis and improves electrophysiological parameters. GLPG0492 prevents immobilization-induced muscle atrophy and regulates muscle mass homeostasis, serving as a valuable tool compound for studies on Duchenne muscular dystrophy, muscle loss and various types of disuse musculoskeletal atrophy[1][2][3][4].
In Vitro:GLPG0492 (10−12-10−5 M) acts as a weak androgen agonist in yeast androgen screening assays, with an EC50 of 1.30 × 10−6 M[1].GLPG0492 (10−11-10−5 M; 24 h) acts as an androgen agonist in human PC3 (AR) 2 prostate cancer cells, with an EC50 of 1.24 × 10−8 M, and this agonistic activity is antagonized by the antiandrogen drug bicalutamide (HY-14249)[1]. In Vivo:GLPG0492 (30 mg/kg; s.c.; once daily, 6 days per week; for 4 consecutive weeks) significantly improves in vivo forelimb strength and exercise endurance in mdx mice after exercise, enhances diaphragmatic contractile function, reduces diaphragmatic fibrosis, and improves the levels of EDL muscle cell injury markers[2].
GLPG0492 (0.3-30 mg/kg; s.c.; once daily, 6 days per week for 12 weeks) significantly enhances long-term forelimb strength and exercise endurance in mdx mice after exercise, improves the functions of the diaphragm and EDL muscle, reduces the degeneration-regeneration cycle and fibrosis of the diaphragm, and ameliorates cell damage markers in the EDL muscle, with a plateau effect often observed at low doses[2].
GLPG0492 (0.3-30 mg/kg; s.c.; 6 days per week; for 4 to 12 weeks) significantly increases forelimb grip strength, maintains running capacity, improves muscle electrophysiological and histological parameters, and exhibits a dose-dependent therapeutic effect in exercised mdx mice (a model of Duchenne muscular dystrophy)[3].
GLPG0492 (0.3-10 mg/kg; s.c.; once daily for 7 consecutive days) dose-dependently alleviates hindlimb immobilization-induced muscle atrophy in male BALB/cj mice; at doses of 3 and 10 mg/kg/day, it exerts maximal improving effects on muscle mass and myofiber size, without causing damage to reproductive tissues, and regulates key muscle atrophy signaling pathways related to mitochondrial bioenergetics and plasma metabolic markers[4].
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- HY-18102
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