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氟他胺 /Flutamide 98%

货号:A208282 同义名: SCH 13521;Niftolide Ambeed 开学季,买赠积分,赢豪礼

Flutamide is a competitive non-steroidal antagonist of androgen receptor.

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Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Flutamide 化学结构 CAS号:13311-84-7
Flutamide 化学结构
CAS号:13311-84-7
Flutamide 3D分子结构
CAS号:13311-84-7
Flutamide 化学结构 CAS号:13311-84-7
Flutamide 3D分子结构 CAS号:13311-84-7
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Flutamide 纯度/质量文件 产品仅供科研

货号:A208282 标准纯度: 98%
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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。

Flutamide 生物活性

靶点
  • Androgen Receptor

    Androgen Receptor, Ki:55 nM

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].

Flutamide 动物研究

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
Animal Rats[6]
Dose 12 mg/kg
Administration i.v.
AUCinf 7.97 ± 0.22 μg·h/ml
Vd 2.31 ± 0.1 L/kg
T1/2 0.88 ± 0.02 h
Tmax 0.25 ± 0.02 h
CL 1.51 ± 0.2 L/h/kg
Cmax 7.10 ± 0.5 μg/ml
MRTinf 1.19 ± 0.2 h

Flutamide 参考文献

[1]Luthy IA, Begin DJ, Labrie F. Androgenic activity of synthetic progestins and spironolactone in androgen-sensitive mouse mammary carcinoma (Shionogi) cells in culture. J Steroid Biochem. 1988 Nov;31(5):845-52.

[2]Simard J, Luthy I, et al. Characteristics of interaction of the antiandrogen flutamide with the androgen receptor in various target tissues. Mol Cell Endocrinol. 1986 Mar;44(3):261-70.

[3]Raghow S, Kuliyev E, et al. Efficacious chemoprevention of primary prostate cancer by flutamide in an autochthonous transgenic model. Cancer Res. 2000 Aug 1;60(15):4093-7.

[4]Pu Y, Xu M, et al. Androgen receptor antagonists compromise T cell response against prostate cancer leading to early tumor relapse. Sci Transl Med. 2016 Apr 6;8(333):333ra47.

[5]Wang HX, Liu X, et al. Induction of liver cytochrome P450 1A2 expression by flutamide in rats. Acta Pharmacol Sin. 2005 Nov;26(11):1382-6.

[6]Elzoghby AO, Helmy MW, et al. Novel ionically crosslinked casein nanoparticles for flutamide delivery: formulation, characterization, and in vivo pharmacokinetics. Int J Nanomedicine. 2013;8:1721-32.

[7]Shukla GC, Plaga AR, Shankar E, Gupta S. Androgen receptor-related diseases: what do we know? Andrology. 2016 May;4(3):366-81. doi: 10.1111/andr.12167. Epub 2016 Mar 16. PMID: 26991422.

[8]Simard J, Luthy I, Guay J, Bélanger A, Labrie F. Characteristics of interaction of the antiandrogen flutamide with the androgen receptor in various target tissues. Mol Cell Endocrinol. 1986 Mar;44(3):261-70. doi: 10.1016/0303-7207(86)90132-2. PMID: 3956856.

[9]Marchetti B, Labrie F. Characteristics of flutamide action on prostatic and testicular functions in the rat. J Steroid Biochem. 1988 Jun;29(6):691-8. doi: 10.1016/0022-4731(88)90170-7. PMID: 2838689.

Flutamide 实验方案

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

Flutamide 技术信息

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

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

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
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