货号:A526563 同义名: N-desmethyl MDV 3100
N-desmethyl Enzalutamide 是 Enzalutamide 的活性代谢物,其主要和次要药效学作用与 Enzalutamide 本身相似,浓度与 Enzalutamide 在血浆中的浓度相当。
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产品名称 | Androgen Receptor ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Cyproterone acetate |
++++
Androgen Receptor, IC50: 7.1 nM |
98% | |||||||||||||||||
Apalutamide |
+++
Androgen Receptor, IC50: 16 nM |
98% | |||||||||||||||||
AZD3514 |
+
Androgen Receptor, Ki: 2.2 μM |
98% | |||||||||||||||||
Darolutamide |
++++
Androgen receptor, Ki: 11 nM |
98% | |||||||||||||||||
Flutamide |
+++
Androgen Receptor, Ki: 55 nM |
98% | |||||||||||||||||
Galeterone |
++
Androgen Receptor, IC50: 384 nM |
98% | |||||||||||||||||
Enzalutamide |
+++
Androgen Receptor, IC50: 36 nM |
98% | |||||||||||||||||
Megestrol | ✔ | 98% | |||||||||||||||||
Bicalutamide |
++
Androgen Receptor, IC50: 0.16 μM |
99% | |||||||||||||||||
EPI-001 |
+
Androgen Receptor, IC50: ~6 μM |
98% | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | N-desmethyl Enzalutamide is an active metabolite of Enzalutamide, demonstrating primary and secondary pharmacodynamics similar in potency to Enzalutamide itself. It circulates in plasma at concentrations comparable to those of Enzalutamide[1]. |
体内研究 | This metabolite is thought to contribute significantly to the clinical effects of Enzalutamide due to its similar pharmacological activity and plasma levels. In contrast, the carboxylic acid metabolite of Enzalutamide is pharmacologically inactive and circulates at plasma concentrations approximately 25% lower than those of Enzalutamide[1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.22mL 0.44mL 0.22mL |
11.10mL 2.22mL 1.11mL |
22.20mL 4.44mL 2.22mL |
CAS号 | 1242137-16-1 |
分子式 | C20H14F4N4O2S |
分子量 | 450.409 |
别名 | N-desmethyl MDV 3100 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Inert atmosphere,Room temperature |
溶解度 |
DMSO: 105 mg/mL(233.12 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |