货号:A208282 同义名: SCH 13521;Niftolide
Flutamide is a competitive non-steroidal antagonist of androgen receptor.
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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。 |
靶点 |
|
描述 | The androgen receptor (AR) and the androgen-AR signaling pathway play a significant role in male sexual differentiation and the development and function of male reproductive and non-reproductive organs [7]. Flutamide, mainly used in the treatment of prostate cancer, is an antiandrogenic drug. Flutamida-OH is the active metabolite form of Flutamide and directly binds to the androgen receptor with Ki of 55 nM. In rat adenohypophysial cells in primary culture, the specific uptake of [3H] testosterone (T) is completely blocked by increasing concentrations of the pure antiandrogen flutamide-OH at an IC50 value of 50 nM [8]. In adult male rats, Treatment for 10 days with flutamide (5 mg/rat, twice daily) caused a marked stimulation of plasma testosterone (T) associated with a significant increase in plasma gonadotropin concentrations and inhibited plasma prolactin (PRL) levels. Moreover, flutamide treatment alone produces an important inhibition of ventral prostate and seminal vesicle weights associated with a significant decrease in prostatic beta-adrenergic receptor levels [9]. |
Dose | Mice: 6.6 mg/kg, 33 mg/kg[3] (s.c.); 60 mg/kg[4] (i.p.) Rat: 50 mg/kg - 200 mg/kg[5] (p.o.); 12 mg/kg[6] (i.v.) | ||||||||||||||||||||
Administration | s.c., i.p. | ||||||||||||||||||||
Pharmacokinetics |
|
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.62mL 0.72mL 0.36mL |
18.10mL 3.62mL 1.81mL |
36.20mL 7.24mL 3.62mL |
CAS号 | 13311-84-7 |
分子式 | C11H11F3N2O3 |
分子量 | 276.21 |
别名 | SCH 13521;Niftolide;Testotard. FLUT.;Tecnoflut;Tafenil;Prostogenat;Prostica;Prostadirex;Prostacur;Profamid;Oncosal;Grisetin;Fugerel;Flutaplex;Flutan;Flutamin;Flutamex;FlutaGry;Flutacan;Flutabene;Flulem;Fluken;Flucinome;Eulexine;Euflex;Drogenil;Chimax;Apimid;Eulexin;Niftolid;Flugerel;Flucinom;NSC 251876;NSC 147834 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,Room Temperature |
溶解度 |
DMSO: 105 mg/mL(380.15 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 |