• 提示：详情请下载说明书。

• 产品描述： ORM-15341 is a potent and full antagonist for human AR (hAR) with IC50 values of 38 nM as shown by transactivation assays in AR-HEK293 cells stably expressing full-length hAR and an androgen-responsive luciferase reporter gene construct. IC50 value: 38 nM Target: androgen receptor in vitro: In competitive AR binding assays, the inhibition constant (Ki) values of ORM-15341 was 8 nM. ORM-15341 functions as a full antagonist for all tested mutant ARs , with IC50 of 25, 51, 700, and 1160 nM for wtAR, AR(F876L), AR(T877A), and AR(W741L).

• 靶点： Androgen Receptor;AndrogenReceptor

• 体外研究：
  The antagonistic properties of the different compounds in a cell - based transactivation assay using an MMT - driven luciferase reporter were determined. For darolutamide, the (S,R)‐ and (S,S)‐diastereomers, and the main in vivo metabolite keto‐darolutamide, a strong antagonistic activity against AR wild type, when stimulating with 1 nM R1881, was found. This was reduced but still significantly better than observed for other AR antagonists when increasing the androgen level used for stimulation to 10 nM. Strong antagonism was also measured for darolutamide, its diastereomers and for keto‐darolutamide when testing the W742C and W742L forms.

• 体内研究：
  The absorption, distribution, metabolism and excretion properties of darolutamide in rats are reported. Keto-darolutamide was the most abundant metabolite in rat hepatocytes and the only major one in plasma. Interconversion between diastereoisomers was observed.

• 参考文献：
  1. Moilanen AM, et al. Discovery of ODM-201, a new-generation androgen receptor inhibitor targeting resistance mechanisms toandrogen signaling-directed prostate cancer therapies. Sci Rep. 2015 Jul 3;5:12007. doi: 10.1038/srep12007. 2. Toermaekangas Olli, et al. Preparation of heteroaryl carboxamides as androgen receptor modulators. From PCT Int. Appl. (2012), WO 2012143599 A1 20121026.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.52 ml	12.6 ml	25.2 ml
  5 mM	0.504 ml	2.52 ml	5.04 ml
  10 mM	0.252 ml	1.26 ml	2.52 ml
  50 mM	0.05 ml	0.252 ml	0.504 ml

• 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。

输入产品批号：

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 *