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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.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $68 | In Stock | |
5 mg | $167 | In Stock | |
10 mg | $248 | In Stock | |
25 mg | $397 | In Stock | |
50 mg | $572 | In Stock | |
100 mg | $768 | In Stock | |
200 mg | $987 | In Stock | |
1 mL x 10 mM (in DMSO) | $178 | In Stock |
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 |
Smiles | CN1C(=O)N(C(=O)[C@@]1(CO)c1ccccc1)c1ccc(C#N)c(c1)C(F)(F)F |
Relative Density. | 1.50 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 45 mg/mL (115.6 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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