标签归档：ospemifene

Ospemifene-d4-1(Synonyms: FC-1271a-d4-1)

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Ospemifene-d4-1 (Synonyms: FC-1271a-d4-1)

Ospemifene-d4-1 (FC-1271a-d4-1) 是 Ospemifene 的氘代物。Ospemifene 是一种非雌激素选择性雌激素受体 (estrogen receptor) 调节剂 (SERM)，对雌激素受体 α (ERα) 和 ERβ 的 Kis 值分别为 380 和 410 nM。Ospemifene 可用于阴道萎缩乳腺癌的研究。

Ospemifene-d4-1(Synonyms: FC-1271a-d4-1)

Ospemifene-d4-1 Chemical Structure

CAS No. : 2734564-80-6

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生物活性

Ospemifene-d4-1 (FC-1271a-d4-1) is the deuterium labeled Ospemifene. Ospemifene is a non-estrogen selective estrogen receptor modulator (SERM), with Kis of 380 and 410 nM for estrogen receptor α (ERα) and ERβ, respectively. Ospemifene can be used for the research of vaginal atrophy and breast cancer[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

382.92

Formula

C24H19D4ClO2
CAS 号

2734564-80-6
中文名称

奥培米芬 d4-1
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]. Qiang Qv.et al.Selective estrogenic effects of a novel triphenylethylene compound, FC1271a, on bone, cholesterol level, and reproductive tissues in intact and ovariectomized rats. Endocrinology.Feb;141(2):809-20. 25. (2000).

    [3]. Tracy L. Taras et al.In vitro and in vivo biologic effects of Ospemifene (FC-1271a) in breast cancer. The Journal of Steroid Biochemistry and Molecular Biology 77(4-5):271-9,(2001).

    [4]. Unkila M, et, al. Vaginal effects of ospemifene in the ovariectomized rat preclinical model of menopause. J Steroid Biochem Mol Biol. 2013 Nov;138:107-15.

    [5]. Bruyniks N, et, al. Systematic indirect comparison of ospemifene versus local estrogens for vulvar and vaginal atrophy. Climacteric. 2017 Jun; 20(3): 195-204.

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