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盐酸萘夫昔定 /Nafoxidine HCl {[allProObj[0].p_purity_real_show]}

货号:A238397

Nafoxidine HCl是一种非甾体选择性雌激素受体调节剂(SERM)或部分抗雌激素,属于三苯乙烯类,已开发用于治疗晚期乳腺癌。

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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+
Nafoxidine HCl 化学结构 CAS号:1847-63-8
Nafoxidine HCl 化学结构
CAS号:1847-63-8
Nafoxidine HCl 3D分子结构
CAS号:1847-63-8
Nafoxidine HCl 化学结构 CAS号:1847-63-8
Nafoxidine HCl 3D分子结构 CAS号:1847-63-8
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Nafoxidine HCl 纯度/质量文件 产品仅供科研

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Nafoxidine HCl 生物活性

描述 Estrogen mediates its action following binding to the estrogen receptor to form an estrogen-receptor complex. The complex initiates gene transcription and produces estrogen-induced cell and/or tissue responses, i.e., estrogenic actions[3]. Estrogen receptor(ER) consists of two subtypes i.e. ERα and ERβ, that are mostly G-protein-coupled receptors and activated by estrogen, specially 17β-estradiol. The activation is followed by translocation into the nucleus and binding with DNA to modulate activities of different genes[4]. Nafoxidine, an antiestrogen, is shown to possess antitumor activity against the Zajdela ascitic hepatoma. Nafoxidine prolonged the survival time of the rats injected with the tumor cells; complete regression of the tumor was observed when rats bearing a 3-day-old tumor were injected with this compound. Nafoxidine (Naf) also showed cytotoxic effects against the hepatoma cells in vitro. Naf competed with the binding of labelled estradiol to the tumor cells[5]. Nafoxidine and MER-25 mimicked the actions of estradiol and decreased adipose tissue lipoprotein lipase (LPL) activity by 75-80%. For adipose tissue LPL activity, both nafoxidine and MER-25 were full estrogen agonists and without antiestrogenic activity. Nafoxidine also mimicked the effects of EB by reducing food intake, body weight, and carcass adiposity in ovariectomized rats[6].

Nafoxidine HCl 参考文献

[1]Coelingh Bennink HJ, Verhoeven C, et al. The use of high-dose estrogens for the treatment of breast cancer. Maturitas. 2017 Jan;95:11-23.

[2]Namba R, Young LJ, et al. Selective estrogen receptor modulators inhibit growth and progression of premalignant lesions in a mouse model of ductal carcinoma in situ. Breast Cancer Res. 2005;7(6):R881-9.

[3]Sk Mahasin Alam,et al. Pharmacophore search for anti-fertility and estrogenic potencies of estrogen analogs. J Mol Model. 2008. 14(11), 1071-82.

[4]Tanmay Saha,et al. Estrogen signaling: An emanating therapeutic target for breast cancer treatment. Eur J Med Chem. 2019. 177, 116-143

[5]A Khar. Nafoxidine possesses antitumor activity against an ascitic hepatoma. Eur J Cancer Clin Oncol. 1986. 22(12), 1475-8.

[6]J M Gray, G N Wade. Food intake, body weight, and adiposity in female rats: actions and interactions of progestins and antiestrogens. Am J Physiol. 1981. 240(5), E474-81.

Nafoxidine HCl 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.16mL

0.43mL

0.22mL

10.82mL

2.16mL

1.08mL

21.64mL

4.33mL

2.16mL

Nafoxidine HCl 技术信息

CAS号1847-63-8
分子式C29H32ClNO2
分子量 462.023
别名
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Inert atmosphere,Room Temperature

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