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Flutamide/氟他胺 {[allProObj[0].p_purity_real_show]}

货号:A208282 同义名: SCH 13521; Niftolide

Flutamide是一种非甾体类雄激素受体(AR)拮抗剂,通过竞争性结合雄激素受体,阻断睾酮和二氢睾酮(DHT)的作用,从而抑制前列腺癌细胞的生长。其活性代谢物2-羟基氟他胺具有更高的AR亲和力,常用于研究前列腺癌,特别是在与GnRH类似物联合使用时效果显著。

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

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/氟他胺 化学结构 CAS号:13311-84-7
Flutamide/氟他胺 化学结构
CAS号:13311-84-7
Flutamide/氟他胺 3D分子结构
CAS号:13311-84-7
Flutamide/氟他胺 化学结构 CAS号:13311-84-7
Flutamide/氟他胺 3D分子结构 CAS号:13311-84-7
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Flutamide/氟他胺 纯度/质量文件 产品仅供科研

货号:A208282 标准纯度: {[allProObj[0].p_purity_real_show]}
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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

99%
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%
Spironolactone ++

Androgen Receptor, IC50: 77 nM

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/氟他胺 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/氟他胺 细胞实验

Cell Line
Concentration Treated Time Description References
HepG2 cells 0.05–300 µM 2 hours To compare the mitochondrial toxicity of flutamide, 2-hydroxyflutamide, and bicalutamide in glucose or galactose-conditioned cells. Flutamide and 2-hydroxyflutamide significantly reduced ATP content in galactose medium, indicating mitochondrial toxicity. Toxicol Sci. 2016 Oct;153(2):341-51.
Mouse primary hepatocytes 10 µM or 50 µM 24 hours FLU elevated Cyp1a1, Cyp1a2, Cyp1b1, Nqo1, and Gsta1 mRNA levels at both 10 and 50 μM, indicating that FLU directly activates the AhR signaling pathway. Biochem Pharmacol. 2016 Nov 1;119:93-104.
HepG2 cells 5 µM, 20 µM, and 100 µM 24 hours FLU significantly increased AhR-dependent luciferase activity at 5 μM and higher concentrations, indicating that FLU can activate AhR. Biochem Pharmacol. 2016 Nov 1;119:93-104.
Hepa-1c1c7 cells 5 µM, 20 µM, and 100 µM 24 hours FLU significantly increased AhR-dependent luciferase activity at 5 μM and higher concentrations, indicating that FLU can activate AhR. Biochem Pharmacol. 2016 Nov 1;119:93-104.
Human keratinocytes (HaCaT) 5 mg/ml 72 hours To investigate the effect of Flutamide on HaCaT cell proliferation, results showed that F-PCL and DF-PCL scaffolds significantly increased HaCaT cell proliferation. FASEB J. 2022 May;36(5):e22310.

Flutamide/氟他胺 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6N C57BL/6N mice Gavage 200 mg/kg Once daily for 28 days After 28 days of FLU treatment, a significant increase in liver weights and liver/body weight ratios was observed, along with elevated bile acid levels in serum and liver, indicating that FLU induced hepatomegaly and disrupted bile acid homeostasis. Biochem Pharmacol. 2016 Nov 1;119:93-104.
BALB/C mice Severe burn wound healing model Topical administration 5 mg/ml Single administration, lasting 28 days To investigate the effect of Flutamide on burn wound healing in mice, results showed that F-PCL scaffolds significantly accelerated wound healing, and DF-PCL scaffolds further promoted wound healing. FASEB J. 2022 May;36(5):e22310.

Flutamide/氟他胺 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/氟他胺 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/氟他胺 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/氟他胺 技术信息

CAS号13311-84-7
分子式C11H11F3N2O3
分子量 276.21
SMILES Code CC(C)C(NC1=CC=C([N+]([O-])=O)C(C(F)(F)F)=C1)=O
MDL No. MFCD00072009
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
InChI Key MKXKFYHWDHIYRV-UHFFFAOYSA-N
Pubchem ID 3397
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry,2-8°C

溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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