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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 |
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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. |
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溶解性：
soluble in DMSO |
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保存条件：
-20℃ |
配置溶液浓度参考：
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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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| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
北京