Toremifene-d6 (Z-Toremifene-d6) citrate 是 Toremifene citrate 的氘代物。Toremifene citrate (Z-Toremifene citrate) 是第二代选择性雌激素受体调节剂，对雌激素受体的 IC50 为 1μM。Toremifene citrate 还可以有效抑制传染性 EBOV Zaire 和 Marburg (MARV)，IC50 分别为 0.07 µM 和 2.6 µM。
货号:ajcx35468
CAS:1246833-71-5
分子式:C32H30D6ClNO8
分子量：604.12
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Toremifene-d6 (Z-Toremifene-d6) citrate is the deuterium labeled Toremifene citrate. Toremifene citrate (Z-Toremifene citrate) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 µM and 2.6 µM, respectively[1][2].

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.
[2]. Matthew R Smith, Selective Estrogen Receptor Modulators to Prevent Treatment-Related Osteoporosis.Rev Urol. 2005; 7(Suppl 3): S30-S35.
[3]. Laura Cooper, et al. Screening and Reverse-Engineering of Estrogen Receptor Ligands as Potent Pan-Filovirus Inhibitors. J Med Chem. 2020 Sep 4.
[4]. Gauri J Sabnis, Luciana Macedo, Olga Goloubeva, Toremifene - Atamestane; Alone or In Combination: Predictions from the Preclinical Intratumoral Aromatase Model. J Steroid Biochem Mol Biol. 2008 January; 108(1-2): 1-7.
[5]. Taneja SS, Morton R, Barnette G, Prostate cancer diagnosis among men with isolated high-grade intraepithelial neoplasia enrolled onto a 3-year prospective phase III clinical trial of oral toremifene. J Clin Oncol. 2013 Feb 10;31(5):523-9.