Nafoxidine HCl

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Chemical Structure| 1847-63-8 同义名 : -
CAS号 : 1847-63-8
货号 : A238397
分子式 : C29H32ClNO2
纯度 : 98%
分子量 : 462.023
MDL号 : MFCD00056572
存储条件：

Pure form Inert atmosphere,Room Temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
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].
实验方案
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
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.