化学名称 : N-[4-硝基-3-(三氟甲基)苯基]-(2S)-3-[4-(乙酰基氨基)苯氧基]-2-羟基-2-甲基丙酰胺
CAS : 401900-40-1
英文名称: Andarine/
英文同义词: OSTARINE
溶解度:Unknown
储存条件:Storage at -20C 2 years
生物活性
Andarine (S-4) is an investigational selective androgen receptor modulator (SARM) for treatment of conditions such as muscle wasting, osteoporosis and benign prostatic hypertrophy,[1] using the non-steroidal androgen antagonist bicalutamide as a lead compound.[2] Andarine is an orally active partial agonist for androgen receptors. It is less potent in both anabolic and androgenic effects than other SARMs. In an animal model of benign prostatic hypertrophy, andarine was shown to reduce prostate weight with similar efficacy to finasteride, but without producing any reduction in muscle mass or anti-androgenic side effects.[3] This suggests that it is able to competitively block binding of dihydrotestosterone to its receptor targets in the prostate gland, but its partial agonist effects at androgen receptors prevent the side effects associated with the anti-androgenic drugs traditionally used for treatment of BPH.[4] Clinical development of Andarine has been abandoned, given in humans it results in a series specific toxic metabolite
参考文献
1. Zilbermint MF,et al. Future Oncol. 2009 Oct;5(8):1211-20. http://www.ncbi.nlm.nih.gov/pubmed/19852734?itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsPanel.Pubmed_RVDocSum&ordinalpos=1 2. Madeddu C,et al. Curr Opin Support Palliat Care. 2009 Dec;3(4):258-62. http://www.ncbi.nlm.nih.gov/pubmed/19667995?itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsPanel.Pubmed_RVDocSum&ordinalpos=2 3.http://www.gtxinc.com/Pipeline/OstarineMK2866.aspx?Sid=4