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Flutamide

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Chemical Structure| 13311-84-7 同义名 : 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
CAS号 : 13311-84-7
货号 : A208282
分子式 : C11H11F3N2O3
纯度 : 98%
分子量 : 276.21
MDL号 : MFCD00072009
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：
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].
实验方案
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
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.