Tamoxifen-d₃ hydrochloride  (Synonyms: 他莫昔芬盐酸盐-d₃; ICI 46474-d₃ hydrochloride; (Z)-Tamoxifen-d₃ hydrochloride; trans-Tamoxifen-d₃ hydrochloride)

Tamoxifen-d₃ hydrochloride is deuterated labeled Tamoxifen (Citrate) (HY-13757). Tamoxifen Citrate (ICI 46474) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells^[1][2][3].Tamoxifen Citrate is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen Citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC₅₀ of 0.1 μM and 1.8 μM, respectively^[5]. Tamoxifen Citrate activates autophagy and induces apoptosis^[4].Tamoxifen Citrate also can induce gene knockout of CreER(T2) transgenic mouse^[6].

氢、碳和其他元素的稳定重同位素已被纳入药物分子中，主要作为药物开发过程中定量的示踪剂。氘化引起了人们的关注，因为它可能影响药物的药代动力学和代谢谱^[1]。
Tamoxifen Citrate (ICI 46474) 对 MCF-7 细胞 (EC₅₀=1.41 μM) 表现出强烈的抑制作用，对 T47D 细胞的抑制作用较小 (EC₅₀=2.5 μM) 但不影响 MDA-MB-231 细胞^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

410.99

C₂₆H₂₇D₃ClNO

他莫昔芬盐酸盐-d₃；三苯氧胺盐酸盐-d₃；它莫西芬盐酸盐-d₃

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216.  [Content Brief]

  [2]. Zhao R, et al. Tamoxifen enhances the Hsp90 molecular chaperone ATPase activity. PLoS One. 2010 Apr 1;5(4):e9934.  [Content Brief]

  [3]. Jia Y, et al. Cardiomyocyte-Specific Ablation of Med1 Subunit of the Mediator Complex Causes Lethal DilatedCardiomyopathy in Mice. PLoS One. 2016 Aug 22;11(8):e0160755.  [Content Brief]

  [4]. Osborne CK. Tamoxifen in the treatment of breast cancer. N Engl J Med. 1998 Nov 26;339(22):1609-18.  [Content Brief]

  [5]. Feil S, et, al. Inducible Cre mice. Methods Mol Biol. 2009;530:343-63.  [Content Brief]

  [6]. Hawariah A, et al. In vitro response of human breast cancer cell lines to the growth-inhibitory effects of styrylpyrone derivative (SPD) and assessment of its antiestrogenicity. Anticancer Res. 1998 Nov-Dec;18(6A):4383-6.  [Content Brief]

  [7]. Laura Cooper, et al. Screening and Reverse-Engineering of Estrogen Receptor Ligands as Potent Pan-Filovirus Inhibitors. J Med Chem. 2020 Sep 4.  [Content Brief]