Toremifene-d6(Synonyms: Z-Toremifene-d6; NK 622-d6 free base; FC-1157a-d6 free base)

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Toremifene-d6 (Synonyms: Z-Toremifene-d6; NK 622-d6 free base; FC-1157a-d6 free base)

Toremifene-d6 是 Toremifene 氘代物。Toremifene (Z-Toremifene) 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 还可以有效抑制传染性 EBOV ZaireMarburg (MARV)IC50 分别为 0.07 µM 和 2.6 µM。

Toremifene-d6(Synonyms: Z-Toremifene-d6; NK 622-d6 free base; FC-1157a-d6 free base)

Toremifene-d6 Chemical Structure

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生物活性

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

体外研究
(In Vitro)

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

412.00

Formula

C26H22D6ClNO

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

参考文献
  • [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.

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