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• 产品描述： 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

• 靶点： Androgen Receptor;AndrogenReceptor

• 体外研究：
  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. 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%). 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

• 参考文献：
  1. Nique F, et al. Identification of a 4-(hydroxymethyl)diarylhydantoin as a selective androgen receptor modulator. J Med Chem. 2012 Oct 11;55(19):8236-47. 2. Blanqué R, et al. Characterization of GLPG0492, a selective androgen receptor modulator, in a mouse model of hindlimb immobilization. BMC Musculoskelet Disord. 2014 Sep 3;15:291. 3. Cozzoli A, et al. GLPG0492, a novel selective androgen receptor modulator, improves muscle performance in the exercised-mdx mouse model of muscular dystrophy. Pharmacol Res. 2013 Jun;72:9-24.

• 溶解性： soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.569 ml	12.843 ml	25.685 ml
  5 mM	0.514 ml	2.569 ml	5.137 ml
  10 mM	0.257 ml	1.284 ml	2.569 ml
  50 mM	0.051 ml	0.257 ml	0.514 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *